TRP Channel
抑制剂选择性比较
TRP Channel产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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E0026New |
ML-SI3ML-SI3 是一种有效的 TRPML通道抑制剂,对 TRPML1 和 TRPML2 的 IC50 分别为 4.7 µM 和 1.7 µM。 |
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E0028New |
9-Phenanthrol9-Phenanthrol(9-Hydroxyphenanthrene, Phenanthren-9-ol, 9-Phenanthrenol)是一种选择性 TRPM4 抑制剂,IC50 为 0.02 μM,对 TRPM5 没有影响。 |
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S2918 |
HC-030031HC-030031 (TOSLAB 829227) 是一种选择性的TRPA1通道阻断剂,可以拮抗AITC和formalin引起的钙流入,IC50分别为6.2μM和5.3μM。 |
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S7999 |
SKF96365SKF96365,最初认为是钙通道阻滞剂,目前作为TRPC通道阻滞剂,被广泛用于医疗诊断。 |
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S8691 |
ML204ML204是新型的、有效的、选择性的TRPC4抑制剂。在胞内钙离子荧光分析试验中,IC50为1 μM。在全细胞电压钳实验中,IC50约为3 μM。ML204对TRPC通道的选择性远高于对其他TRP通道和非TRP通道的选择性。 |
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S9140 |
PulegonePulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient. |
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S0750 |
GFB-8438GFB-8438 是一种新型的、有效的、具有亚型选择性的 TRP channel subfamily C (TRPC) 的抑制剂,对于 TRPC4 和 TRPC5 的IC50值分别为0.18 μM和0.29 μM,并且显示出对TRPC6、其他TRP家族成员、NaV 1.5的出色选择性,以及对 hERG channel的有限活性。 |
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S0977 |
AC1903AC1903 (compound 2) 是一种特异性、选择性的 TRPC5 (transient receptor potential canonical channel 5) 的抑制剂,IC50值为 4.06 μM。 |
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S6634 |
SAR7334SAR7334是一种新型,高效且可生物利用的TRPC6通道抑制剂。SAR7334在膜片钳实验中阻断了TRPC6电流,IC50为7.9 nM。 |
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S2277 |
Caffeic AcidCaffeic Acid是一种羟基肉桂酸,是一种天然存在的有机化合物。 |
![]() ![]() Validation of caffeic acid phenethyl ether (CAPE) activity in LPS cells. T778 cells were transfected with either HOXA5 expression vector or empty vector control. Cells were treated with 25 μg/ml CAPE 9 h after transfection, incubated for an additional 15 h, and subjected to Western blotting. Representative images are shown. HNRNPA1 and TUBA4A (α-tubulin) were used as loading control for nuclear (N) and cytoplasmic (C) fraction of cells, respectively. Numbers indicate relative band intensity of RELA normalized to the intensity of the genes in control (1.0) for each fraction.
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S6070 |
CBA (TRPM4-IN-5)CBA (TRPM4-IN-5, Compound 5) 是 TRPM4 离子通道的高选择性阻断剂,IC50 为 1.5μM。 |
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S8367 |
GSK2193874GSK2193874是一种具有口服活性的、有效的、选择性transient receptor potential vanilloid 4 (TRPV4)阻滞剂,对hTRPV4和rTRPV4的IC50分别为0.04和0.002 μM。 |
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S6410 |
ClemizoleClemizole是第一代组胺受体(H1 receptor)拮抗剂,是有效的行为性和电生理癫痫活性的抑制剂。它对丙型肝炎的感染具有潜在疗效,能有效地抑制TRPC5离子通道。 |
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S9926New |
ML-SA1ML-SA1(Mucolipin synthetic agonist 1)是一种选择性 TRPML通道 的激动剂。ML-SA1可通过促进溶酶体的酸化和蛋白酶活性,抑制登革病毒2型(DENV2) 和寨卡病毒(ZIKV)。ML-SA1 抗 DENV2 RNA 和 ZIKV RNA 的 IC50 值分别为 8.93 μM 和 52.99 μM。ML-SA1 可诱发自噬。ML-SA1也可用于广谱抗病毒研究。 |
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S7848New |
QX-314 chlorideQX-314 chloride 通过直接激活并渗透 TRPV1 和 TRPA1 ,从而抑制 钠通道 (sodium channels)。 |
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S6947New |
MK6-83MK6-83 是一种新型的 Transient receptor potential melastatin member 1 (TRPML1) 的激活剂,可用作 MLIV 患者特定亚组的潜在药物治疗选择。 |
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S8639 |
Diphenyleneiodonium chloride (DPI)Diphenyleneiodonium chloride (DPI)是 NADPH oxidase 的抑制剂,也是有效的、不可逆的 iNOS/eNOS 抑制剂。Diphenyleneiodonium chloride (DPI) 还起到 TRPA1 激活剂的作用,并能选择性地抑制细胞内的活性氧(ROS)。 |
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S8073 |
OptovinOptovin是一个可逆的光活化的TRPA1活化剂。 |
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S6657 |
2-Aminoethyl Diphenylborinate (2-APB)2-Aminoethyl Diphenylborinate (2-APB)是IP3 receptor的抑制剂,可以调节IP3诱导的钙释放。2-APB还可以抑制SOC通道的活性,并且在高浓度的时候可以激活TRP通道。 |
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S8107 |
GSK1016790AGSK1016790A (GSK101)是一种新型的、有效的TRPV4激活剂,其在人脉络丛上皮细胞中的EC50为34 nM。 |
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S5419 |
1,4-Cineole1,4-Cineole (Isocineole) is a flavor constituent of Citrus aurantifolia and Piper cubeba. |
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S3851 |
CamphorCamphor (2-Bornanone, Bornan-2-one, 2-Camphanone, Formosa) is a bicyclic monoterpene ketone found widely in plants, especially cinnamomum camphora and used topically as a skin antipruritic and as an anti-infective agent. |
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S4516 |
(+)-CamphorCamphor是一种蜡质的、易燃的、白色或透明的固体,有强烈的香味,通常用于缓解疼痛、减少瘙痒以及治疗真菌感染。它能够激活TRPV1和TRPV3。 |
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S4714 |
(-)-Menthol(-)-Menthol (L-Menthol, Levomenthol, Menthomenthol, Menthacamphor) 是薄荷醇的左旋异构体,常被用作冷却剂,可激活TRPM8。 |
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S2773 |
SB705498SB705498是一种hTRPV1拮抗剂,抑制TRPV1的Capsaicin,酸和热激活,IC50分别为3 nM, 0.1 nM和6 nM,该作用具有一定的电压依赖性,作用于TRPV1比作用于TRPM8选择性高100倍以上。Phase 2。 |
![]() ![]() (B) SK-N-SH cells were incubated with AM251 (CB1 antagonist) or SB705498 (TRPV-1 antagonist) for 30 min and stimulated with NADA (10 μM) for 6 h. The expression of HIF-1α protein was determined by immunoblot analysis. We show a representative blot of three independent experiments. |
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S7115 |
AMG-517AMG-517是一种有效的,选择性的TRPV1拮抗剂,抑制TRPV1的Capsaicin, Proton和热激活,IC50分别为0.76 nM, 0.62 nM和1.3 nM。 |
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S3942 |
CardamoninCardamonin (Alpinetin chalcone)天然存在于良姜属物种的果实中,具有抗炎和抗肿瘤活性。它是一种新型的hTRPA1离子通道拮抗剂,IC50为454 nM,而不与TRPV1和TRPV4相互作用。 |
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S6638 |
AMG-333AMG-333是有效的、高选择性的TRPM8拮抗剂,对人源TRPM8和大鼠TRPM8的IC50值分别为13 nM和30 nM。 |
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S6637 |
HC-067047HC-067047是一种选择性的TRPV4拮抗剂,对人TRPV4,大鼠TRPV4和小鼠TRPV4的IC50分别为48 nM,133 nM和17 nM。 |
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S8137 |
CapsazepineCapsazepine是capsaicin的拮抗剂,是TRPV1的拮抗剂。 |
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S3756 |
Methyl salicylateMethyl salicylate (Betula oil, Gaultheria oil, Methyl 2-hydroxybenzoate, Natural wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1. |
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S6934 |
AMG-9810AMG-9810 是一种有效的、竞争性和选择性的 vanilloid receptor 1 (TRPV1) 的拮抗剂,可抑制辣椒素capsaicin的活化,对人TRPV1和大鼠TRPV1的IC50值分别为24.5 nM和85.6 nM。AMG-9810 可阻止所有已知模式的TRPV1激活,包括protons-,heat-和endogenous ligands,例如anandamide,N-arachidonyl dopamine和oleoyldopamine。AMG-9810 可显著降低 TLR2 和 TLR4 的mRNA表达。AMG-9810 还可通过 EGFR/Akt/mTOR 信号通路来促进小鼠皮肤肿瘤发生的缓解。 |
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S6838 |
BCTCBCTC 是一种口服的、高效的 vanilloid receptor 1 (VR1/TRPV1) 的拮抗剂。BCTC 对于辣椒素诱导和酸诱导的大鼠VR1活化的IC50值分别为35 nM和6.0 nM。BCTC 具有抗肿瘤的活性。 |
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S0174 |
TRPM8 antagonist 2TRPM8 antagonist 2 (TRPM8 Antagonist)是一种有效的 TRPM8 的拮抗剂,IC50值为0.2 nM,可用于神经性疼痛综合征的药理治疗。 |
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S8238 |
SB366791SB-366791是一种新型有效的选择性TRPV1拮抗剂。IC50为5.7 nM。 |
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S3867 |
(E)-Cardamonin(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor. |
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S2650 |
RN-1734RN-1734 (TRPV4 Antagonist I)是一种选择性的 transient receptor potential vanilloid 4 (TRPV4) 拮抗剂,对于hTRPV4、mTRPV4和rTRPV4的IC50值分别为2.3 μM、5.9 μM和3.2 μM。RN-1734 在不改变olig2阳性细胞数量的情况下,可减轻脱髓鞘作用并抑制神经胶质活化以及抑制 tumor necrosis factor α (TNF-α) 和 interleukin 1β (IL-1β) 的产生。 |
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S4022 |
ProbenecidProbenecid (Benemid)是一种经典的有机阴离子运输竞争性抑制剂,同时也是一种瞬时感受器电位香草素受体亚家族2(TRPV2)的激动剂和人苦味觉感受器TAS2R16的抑制剂。Probenecid 还可以抑制Pannexin1 (Panx1)通道。 |
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E0031New |
RN-1747RN-1747 是一种选择性 TRPV4 激动剂,对 hTRPV4、mTRPV4 和 rTRPV4 的 EC50 分别为 0.77 μM、4.0 μM 和 4.1 μM。RN-1747还拮抗 TRPM8,IC50 为 4 μM。 |
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S6122 |
CyclohexanecarboxamideCyclohexanecarboxamide (Ethyl menthane carboxamide, WS3, Hexahydrobenzamide)是一种制冷剂,也是TRPM8受体激动剂,EC50为3.7 μM。 |
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S0825 |
MDR-652MDR-652 是一种有效的 transient receptor potential vanilloid 1 (TRPV1) 的特异性激动剂,对hTRPV1和rTRPV1的Ki值分别为11.4 nM和23.8 nM。MDR-652 具有出色的剂量依赖性的镇痛作用。 |
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S3763 |
CinnamaldehydeCinnamaldehyde is a flavonoid that is naturally synthesized by the shikimate pathway. Its supplementation can improve glucose and lipid homeostasis in diabetic animals; a TRPA1 agonist. |
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S1990 |
Capsaicin(Vanilloid)Capsaicin (Qutenza, Vanilloid) 是辣椒属红辣椒的活性成分。 |
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S3935 |
NonivamideNonivamide (pelargonic acid vanillylamide, Pseudocapsaicin, Vanillyl-N-nonylamide), present in chili peppers, is commonly manufactured synthetically and used as a food additive to add pungency to seasonings, flavorings, and spice blends. |
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S9086 |
DihydrocapsaicinDihydrocapsaicin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical. |
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S3605 |
BorneolBorneol是一种分离自药用植物如艾纳香、芳味冰片香木的双环类单萜化合物。它是TRPM8的激动剂,能够增加眼部表面湿润。 |
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S4787 |
Methyl syringateMethyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist. |
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S2963 |
WS-12WS-12 是一种有效的 TRPM8 激动剂,EC50 为 39 nM。 |
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S2505 |
Rosiglitazone (BRL-49653) maleateRosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药,是PPARγ的高亲和、选择性的激动剂,IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。 |
![]() ![]() Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast. |
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S2556 |
Rosiglitazone (BRL 49653)Rosiglitazone (BRL 49653) 是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。 |
![]() ![]() |
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S6409 |
ZucapsaicinZucapsaicin是capsaicin的顺式异构体,是一种局部镇痛剂,用于治疗膝骨关节炎和其他神经痛。它是一种TRPV-1调节剂。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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E0026New |
ML-SI3ML-SI3 是一种有效的 TRPML通道抑制剂,对 TRPML1 和 TRPML2 的 IC50 分别为 4.7 µM 和 1.7 µM。 |
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E0028New |
9-Phenanthrol9-Phenanthrol(9-Hydroxyphenanthrene, Phenanthren-9-ol, 9-Phenanthrenol)是一种选择性 TRPM4 抑制剂,IC50 为 0.02 μM,对 TRPM5 没有影响。 |
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S2918 |
HC-030031HC-030031 (TOSLAB 829227) 是一种选择性的TRPA1通道阻断剂,可以拮抗AITC和formalin引起的钙流入,IC50分别为6.2μM和5.3μM。 |
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S7999 |
SKF96365SKF96365,最初认为是钙通道阻滞剂,目前作为TRPC通道阻滞剂,被广泛用于医疗诊断。 |
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S8691 |
ML204ML204是新型的、有效的、选择性的TRPC4抑制剂。在胞内钙离子荧光分析试验中,IC50为1 μM。在全细胞电压钳实验中,IC50约为3 μM。ML204对TRPC通道的选择性远高于对其他TRP通道和非TRP通道的选择性。 |
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S9140 |
PulegonePulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient. |
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S0750 |
GFB-8438GFB-8438 是一种新型的、有效的、具有亚型选择性的 TRP channel subfamily C (TRPC) 的抑制剂,对于 TRPC4 和 TRPC5 的IC50值分别为0.18 μM和0.29 μM,并且显示出对TRPC6、其他TRP家族成员、NaV 1.5的出色选择性,以及对 hERG channel的有限活性。 |
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S0977 |
AC1903AC1903 (compound 2) 是一种特异性、选择性的 TRPC5 (transient receptor potential canonical channel 5) 的抑制剂,IC50值为 4.06 μM。 |
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S6634 |
SAR7334SAR7334是一种新型,高效且可生物利用的TRPC6通道抑制剂。SAR7334在膜片钳实验中阻断了TRPC6电流,IC50为7.9 nM。 |
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S2277 |
Caffeic AcidCaffeic Acid是一种羟基肉桂酸,是一种天然存在的有机化合物。 |
![]() ![]() Validation of caffeic acid phenethyl ether (CAPE) activity in LPS cells. T778 cells were transfected with either HOXA5 expression vector or empty vector control. Cells were treated with 25 μg/ml CAPE 9 h after transfection, incubated for an additional 15 h, and subjected to Western blotting. Representative images are shown. HNRNPA1 and TUBA4A (α-tubulin) were used as loading control for nuclear (N) and cytoplasmic (C) fraction of cells, respectively. Numbers indicate relative band intensity of RELA normalized to the intensity of the genes in control (1.0) for each fraction.
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S6070 |
CBA (TRPM4-IN-5)CBA (TRPM4-IN-5, Compound 5) 是 TRPM4 离子通道的高选择性阻断剂,IC50 为 1.5μM。 |
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S8367 |
GSK2193874GSK2193874是一种具有口服活性的、有效的、选择性transient receptor potential vanilloid 4 (TRPV4)阻滞剂,对hTRPV4和rTRPV4的IC50分别为0.04和0.002 μM。 |
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S6410 |
ClemizoleClemizole是第一代组胺受体(H1 receptor)拮抗剂,是有效的行为性和电生理癫痫活性的抑制剂。它对丙型肝炎的感染具有潜在疗效,能有效地抑制TRPC5离子通道。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S9926New |
ML-SA1ML-SA1(Mucolipin synthetic agonist 1)是一种选择性 TRPML通道 的激动剂。ML-SA1可通过促进溶酶体的酸化和蛋白酶活性,抑制登革病毒2型(DENV2) 和寨卡病毒(ZIKV)。ML-SA1 抗 DENV2 RNA 和 ZIKV RNA 的 IC50 值分别为 8.93 μM 和 52.99 μM。ML-SA1 可诱发自噬。ML-SA1也可用于广谱抗病毒研究。 |
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S7848New |
QX-314 chlorideQX-314 chloride 通过直接激活并渗透 TRPV1 和 TRPA1 ,从而抑制 钠通道 (sodium channels)。 |
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S6947New |
MK6-83MK6-83 是一种新型的 Transient receptor potential melastatin member 1 (TRPML1) 的激活剂,可用作 MLIV 患者特定亚组的潜在药物治疗选择。 |
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S8639 |
Diphenyleneiodonium chloride (DPI)Diphenyleneiodonium chloride (DPI)是 NADPH oxidase 的抑制剂,也是有效的、不可逆的 iNOS/eNOS 抑制剂。Diphenyleneiodonium chloride (DPI) 还起到 TRPA1 激活剂的作用,并能选择性地抑制细胞内的活性氧(ROS)。 |
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S8073 |
OptovinOptovin是一个可逆的光活化的TRPA1活化剂。 |
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S6657 |
2-Aminoethyl Diphenylborinate (2-APB)2-Aminoethyl Diphenylborinate (2-APB)是IP3 receptor的抑制剂,可以调节IP3诱导的钙释放。2-APB还可以抑制SOC通道的活性,并且在高浓度的时候可以激活TRP通道。 |
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S8107 |
GSK1016790AGSK1016790A (GSK101)是一种新型的、有效的TRPV4激活剂,其在人脉络丛上皮细胞中的EC50为34 nM。 |
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S5419 |
1,4-Cineole1,4-Cineole (Isocineole) is a flavor constituent of Citrus aurantifolia and Piper cubeba. |
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S3851 |
CamphorCamphor (2-Bornanone, Bornan-2-one, 2-Camphanone, Formosa) is a bicyclic monoterpene ketone found widely in plants, especially cinnamomum camphora and used topically as a skin antipruritic and as an anti-infective agent. |
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S4516 |
(+)-CamphorCamphor是一种蜡质的、易燃的、白色或透明的固体,有强烈的香味,通常用于缓解疼痛、减少瘙痒以及治疗真菌感染。它能够激活TRPV1和TRPV3。 |
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S4714 |
(-)-Menthol(-)-Menthol (L-Menthol, Levomenthol, Menthomenthol, Menthacamphor) 是薄荷醇的左旋异构体,常被用作冷却剂,可激活TRPM8。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S2773 |
SB705498SB705498是一种hTRPV1拮抗剂,抑制TRPV1的Capsaicin,酸和热激活,IC50分别为3 nM, 0.1 nM和6 nM,该作用具有一定的电压依赖性,作用于TRPV1比作用于TRPM8选择性高100倍以上。Phase 2。 |
![]() ![]() (B) SK-N-SH cells were incubated with AM251 (CB1 antagonist) or SB705498 (TRPV-1 antagonist) for 30 min and stimulated with NADA (10 μM) for 6 h. The expression of HIF-1α protein was determined by immunoblot analysis. We show a representative blot of three independent experiments. |
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S7115 |
AMG-517AMG-517是一种有效的,选择性的TRPV1拮抗剂,抑制TRPV1的Capsaicin, Proton和热激活,IC50分别为0.76 nM, 0.62 nM和1.3 nM。 |
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S3942 |
CardamoninCardamonin (Alpinetin chalcone)天然存在于良姜属物种的果实中,具有抗炎和抗肿瘤活性。它是一种新型的hTRPA1离子通道拮抗剂,IC50为454 nM,而不与TRPV1和TRPV4相互作用。 |
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S6638 |
AMG-333AMG-333是有效的、高选择性的TRPM8拮抗剂,对人源TRPM8和大鼠TRPM8的IC50值分别为13 nM和30 nM。 |
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S6637 |
HC-067047HC-067047是一种选择性的TRPV4拮抗剂,对人TRPV4,大鼠TRPV4和小鼠TRPV4的IC50分别为48 nM,133 nM和17 nM。 |
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S8137 |
CapsazepineCapsazepine是capsaicin的拮抗剂,是TRPV1的拮抗剂。 |
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S3756 |
Methyl salicylateMethyl salicylate (Betula oil, Gaultheria oil, Methyl 2-hydroxybenzoate, Natural wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1. |
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S6934 |
AMG-9810AMG-9810 是一种有效的、竞争性和选择性的 vanilloid receptor 1 (TRPV1) 的拮抗剂,可抑制辣椒素capsaicin的活化,对人TRPV1和大鼠TRPV1的IC50值分别为24.5 nM和85.6 nM。AMG-9810 可阻止所有已知模式的TRPV1激活,包括protons-,heat-和endogenous ligands,例如anandamide,N-arachidonyl dopamine和oleoyldopamine。AMG-9810 可显著降低 TLR2 和 TLR4 的mRNA表达。AMG-9810 还可通过 EGFR/Akt/mTOR 信号通路来促进小鼠皮肤肿瘤发生的缓解。 |
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S6838 |
BCTCBCTC 是一种口服的、高效的 vanilloid receptor 1 (VR1/TRPV1) 的拮抗剂。BCTC 对于辣椒素诱导和酸诱导的大鼠VR1活化的IC50值分别为35 nM和6.0 nM。BCTC 具有抗肿瘤的活性。 |
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S0174 |
TRPM8 antagonist 2TRPM8 antagonist 2 (TRPM8 Antagonist)是一种有效的 TRPM8 的拮抗剂,IC50值为0.2 nM,可用于神经性疼痛综合征的药理治疗。 |
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S8238 |
SB366791SB-366791是一种新型有效的选择性TRPV1拮抗剂。IC50为5.7 nM。 |
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S3867 |
(E)-Cardamonin(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor. |
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S2650 |
RN-1734RN-1734 (TRPV4 Antagonist I)是一种选择性的 transient receptor potential vanilloid 4 (TRPV4) 拮抗剂,对于hTRPV4、mTRPV4和rTRPV4的IC50值分别为2.3 μM、5.9 μM和3.2 μM。RN-1734 在不改变olig2阳性细胞数量的情况下,可减轻脱髓鞘作用并抑制神经胶质活化以及抑制 tumor necrosis factor α (TNF-α) 和 interleukin 1β (IL-1β) 的产生。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S4022 |
ProbenecidProbenecid (Benemid)是一种经典的有机阴离子运输竞争性抑制剂,同时也是一种瞬时感受器电位香草素受体亚家族2(TRPV2)的激动剂和人苦味觉感受器TAS2R16的抑制剂。Probenecid 还可以抑制Pannexin1 (Panx1)通道。 |
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E0031New |
RN-1747RN-1747 是一种选择性 TRPV4 激动剂,对 hTRPV4、mTRPV4 和 rTRPV4 的 EC50 分别为 0.77 μM、4.0 μM 和 4.1 μM。RN-1747还拮抗 TRPM8,IC50 为 4 μM。 |
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S6122 |
CyclohexanecarboxamideCyclohexanecarboxamide (Ethyl menthane carboxamide, WS3, Hexahydrobenzamide)是一种制冷剂,也是TRPM8受体激动剂,EC50为3.7 μM。 |
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S0825 |
MDR-652MDR-652 是一种有效的 transient receptor potential vanilloid 1 (TRPV1) 的特异性激动剂,对hTRPV1和rTRPV1的Ki值分别为11.4 nM和23.8 nM。MDR-652 具有出色的剂量依赖性的镇痛作用。 |
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S3763 |
CinnamaldehydeCinnamaldehyde is a flavonoid that is naturally synthesized by the shikimate pathway. Its supplementation can improve glucose and lipid homeostasis in diabetic animals; a TRPA1 agonist. |
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S1990 |
Capsaicin(Vanilloid)Capsaicin (Qutenza, Vanilloid) 是辣椒属红辣椒的活性成分。 |
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S3935 |
NonivamideNonivamide (pelargonic acid vanillylamide, Pseudocapsaicin, Vanillyl-N-nonylamide), present in chili peppers, is commonly manufactured synthetically and used as a food additive to add pungency to seasonings, flavorings, and spice blends. |
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S9086 |
DihydrocapsaicinDihydrocapsaicin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical. |
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S3605 |
BorneolBorneol是一种分离自药用植物如艾纳香、芳味冰片香木的双环类单萜化合物。它是TRPM8的激动剂,能够增加眼部表面湿润。 |
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S4787 |
Methyl syringateMethyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist. |
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S2963 |
WS-12WS-12 是一种有效的 TRPM8 激动剂,EC50 为 39 nM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S2505 |
Rosiglitazone (BRL-49653) maleateRosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药,是PPARγ的高亲和、选择性的激动剂,IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。 |
![]() ![]() Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast. |
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S2556 |
Rosiglitazone (BRL 49653)Rosiglitazone (BRL 49653) 是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。 |
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S6409 |
ZucapsaicinZucapsaicin是capsaicin的顺式异构体,是一种局部镇痛剂,用于治疗膝骨关节炎和其他神经痛。它是一种TRPV-1调节剂。 |