TRP Channel

抑制剂选择性比较

TRP Channel产品

所有产品 TRP Channel抑制剂(8) TRP Channel激活剂(8) TRP Channel拮抗剂(11) TRP Channel激动剂(8) TRP Channel调节剂(3)

目录号	产品描述	文献引用	实验数据
S6634^New	SAR7334 SAR7334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。
S2918	HC-030031 HC-030031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。	J Pain, 2019, S1526-5900(19)30794-1
S7999	SKF96365 SKF96365，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。	Mol Med Rep, 2020, 21(2):806-814 Biosci Rep, 2019, 39(1)
S8691	ML204 ML204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。	Nature, 2019, 567(7747):262-266
S9140	Pulegone Pulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient.
S2277	Caffeic Acid Caffeic Acid是一种羟基肉桂酸，是一种天然存在的有机化合物。	J Nutr Biochem, 2015, 26(11):1379-84 Sci Rep, 2015, 5:12580	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.
S8367	GSK2193874 GSK2193874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。	Am J Physiol Lung Cell Mol Physiol, 2019, 317(5):L639-L652 Am J Physiol Lung Cell Mol Physiol, 2018, 314(5):L893-L907
S6410	Clemizole Clemizole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。
S6657^New	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。
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)。	Theranostics, 2020, 10(15):6743-6757 Clin Exp Allergy, 2020, 50(2):198-212 Int J Biochem Cell Biol, 2020, 121:105703
S8073	Optovin Optovin是一个可逆的光活化的TRPA1活化剂。
S8107	GSK1016790A GSK1016790A (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。	Neurosci Lett, 2019, 10.1016/j.neulet.2019.134630
S5419	1,4-Cineole 1,4-Cineole is a flavor constituent of Citrus aurantifolia and Piper cubeba.
S3851	Camphor Camphor 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.
S4516	(+)-Camphor Camphor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。
S4714	(-)-Menthol (-)-Menthol是薄荷醇的左旋异构体，常被用作冷却剂，可激活TRPM8。
S2773	SB705498 SB705498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。	Biogerontology, 2016, 17(5-6):907-920 Biochim Biophys Acta, 2014, 10.1016/j.bbamcr.2014.07.005	(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.
S7115	AMG-517 AMG-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。	Inflammation, 2019, 10.1007/s10753-019-01040-y Mol Pain, 2018, 14:1744806918777614 Anesthesiology, 2017, 127(5):813-823
S6838^New	BCTC BCTC 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。
S2650^New	RN-1734 RN-1734 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。
S6637^New	HC-067047 HC-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。
S6638^New	AMG-333 AMG-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。
S3942	Cardamonin Cardamonin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。
S8137	Capsazepine Capsazepine是capsaicin的拮抗剂，是TRPV1的拮抗剂。	Hum Mol Genet, 2020, 29(2):228-237 Eur J Med Chem, 2019, 168:146-153
S3756	Methyl salicylate Methyl salicylate is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1.
S8238	SB366791 SB-366791是一种新型有效的选择性TRPV1拮抗剂。IC50为5.7 nM。	Mol Pain, 2018, 14:1744806918816850
S3867	(E)-Cardamonin Cardamonin 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.
S4022	Probenecid Probenecid 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。
S6122	Cyclohexanecarboxamide Cyclohexanecarboxamide是一种制冷剂，也是TRPM8受体激动剂，EC50为3.7 μM。
S3763	Cinnamaldehyde Cinnamaldehyde 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.
S1990	Capsaicin(Vanilloid) Capsaicin是辣椒属红辣椒的活性成分。	J Leukoc Biol, 2020, 10.1002/JLB.3MA0220-355R Inflammation, 2019, 10.1007/s10753-019-01040-y Acta Pharmacol Sin, 2018, 39(3):438-448
S3935	Nonivamide Nonivamide, present in chili peppers, is commonly manufactured synthetically and used as a food additive to add pungency to seasonings, flavorings, and spice blends.
S9086	Dihydrocapsaicin Dihydrocapsaicin, found in pepper (C. annuum), is a potential nutriceutical.
S3605	Borneol Borneol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。
S4787	Methyl syringate Methyl syringate, a plant phenolic compound, is a specific and selective TRPA1 agonist.
S2505	Rosiglitazone maleate Rosiglitazone maleate 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。	Virol Sin, 2019, 34(6):648-661 Drugs R D, 2017, 10.1007/s40268-016-0166-4 J Inflamm (Lond), 2016, 13:19	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.
S2556	Rosiglitazone Rosiglitazone 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。	Nat Commun, 2020, 11(1):71 Cancer Cell Int, 2020, 19;20:58 Cancer Chemother Pharmacol, 2020, 85(2):273-284
S6409	Zucapsaicin Zucapsaicin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
S6634^New	SAR7334 SAR7334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。
S2918	HC-030031 HC-030031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。	J Pain,2019, S1526-5900(19)30794-1
S7999	SKF96365 SKF96365，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。	Mol Med Rep,2020, 21(2):806-814 Biosci Rep,2019, 39(1)
S8691	ML204 ML204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。	Nature,2019, 567(7747):262-266
S9140	Pulegone Pulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient.
S2277	Caffeic Acid Caffeic Acid是一种羟基肉桂酸，是一种天然存在的有机化合物。	J Nutr Biochem,2015, 26(11):1379-84 Sci Rep,2015, 5:12580	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.
S8367	GSK2193874 GSK2193874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。	Am J Physiol Lung Cell Mol Physiol,2019, 317(5):L639-L652 Am J Physiol Lung Cell Mol Physiol,2018, 314(5):L893-L907
S6410	Clemizole Clemizole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
S6657^New	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。
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)。	Theranostics, 2020, 10(15):6743-6757 Clin Exp Allergy, 2020, 50(2):198-212 Int J Biochem Cell Biol, 2020, 121:105703
S8073	Optovin Optovin是一个可逆的光活化的TRPA1活化剂。
S8107	GSK1016790A GSK1016790A (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。	Neurosci Lett, 2019, 10.1016/j.neulet.2019.134630
S5419	1,4-Cineole 1,4-Cineole is a flavor constituent of Citrus aurantifolia and Piper cubeba.
S3851	Camphor Camphor 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.
S4516	(+)-Camphor Camphor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。
S4714	(-)-Menthol (-)-Menthol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
S2773	SB705498 SB705498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。	Biogerontology, 2016, 17(5-6):907-920 Biochim Biophys Acta, 2014, 10.1016/j.bbamcr.2014.07.005	(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.
S7115	AMG-517 AMG-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。	Inflammation, 2019, 10.1007/s10753-019-01040-y Mol Pain, 2018, 14:1744806918777614 Anesthesiology, 2017, 127(5):813-823
S6838^New	BCTC BCTC 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。
S2650^New	RN-1734 RN-1734 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。
S6637^New	HC-067047 HC-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。
S6638^New	AMG-333 AMG-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。
S3942	Cardamonin Cardamonin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。
S8137	Capsazepine Capsazepine是capsaicin的拮抗剂，是TRPV1的拮抗剂。	Hum Mol Genet, 2020, 29(2):228-237 Eur J Med Chem, 2019, 168:146-153
S3756	Methyl salicylate Methyl salicylate is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1.
S8238	SB366791 SB-366791是一种新型有效的选择性TRPV1拮抗剂。IC50为5.7 nM。	Mol Pain, 2018, 14:1744806918816850
S3867	(E)-Cardamonin Cardamonin 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.

目录号	产品描述	文献引用
S4022	Probenecid Probenecid 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。
S6122	Cyclohexanecarboxamide Cyclohexanecarboxamide是一种制冷剂，也是TRPM8受体激动剂，EC50为3.7 μM。
S3763	Cinnamaldehyde Cinnamaldehyde 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.
S1990	Capsaicin(Vanilloid) Capsaicin是辣椒属红辣椒的活性成分。	J Leukoc Biol, 2020, 10.1002/JLB.3MA0220-355R Inflammation, 2019, 10.1007/s10753-019-01040-y Acta Pharmacol Sin, 2018, 39(3):438-448
S3935	Nonivamide Nonivamide, present in chili peppers, is commonly manufactured synthetically and used as a food additive to add pungency to seasonings, flavorings, and spice blends.
S9086	Dihydrocapsaicin Dihydrocapsaicin, found in pepper (C. annuum), is a potential nutriceutical.
S3605	Borneol Borneol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。
S4787	Methyl syringate Methyl syringate, a plant phenolic compound, is a specific and selective TRPA1 agonist.

目录号	产品描述	文献引用	实验数据
S2505	Rosiglitazone maleate Rosiglitazone maleate 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。	Virol Sin, 2019, 34(6):648-661 Drugs R D, 2017, 10.1007/s40268-016-0166-4 J Inflamm (Lond), 2016, 13:19	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.
S2556	Rosiglitazone Rosiglitazone 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。	Nat Commun, 2020, 11(1):71 Cancer Cell Int, 2020, 19;20:58 Cancer Chemother Pharmacol, 2020, 85(2):273-284
S6409	Zucapsaicin Zucapsaicin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

S2505

Rosiglitazone maleate

Rosiglitazone maleate 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。

Virol Sin, 2019, 34(6):648-661

Drugs R D, 2017, 10.1007/s40268-016-0166-4

J Inflamm (Lond), 2016, 13:19

S2556

Rosiglitazone

Rosiglitazone 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。

Nat Commun, 2020, 11(1):71

Cancer Cell Int, 2020, 19;20:58

Cancer Chemother Pharmacol, 2020, 85(2):273-284

S6409

Zucapsaicin

Zucapsaicin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。

研究领域

产品类型

TRP Channel

抑制剂选择性比较

TRP Channel产品