NOS

抑制剂选择性比较

NOS产品

目录号 产品描述 文献引用 实验数据
S2877

L-NAME HCl

L-NAME HCl是一种无选择性的一氧化氮合成酶抑制剂,对nNOS (牛源), eNOS (人源)和iNOS (鼠源)的Ki值分别为15nM, 39 nM和4.4 μM。

S9208

Ginsenoside Rb3

Ginsenoside Rb3 是从人参中提取的天然产物,在心血管疾病包括心肌的缺血/再灌注(I/R)损伤中起着重要作用。在人肾293T细胞中检测了Ginsenoside Rb3(0.1-10 μM)对肿瘤坏死因子TNF-α诱导的 nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) 荧光素酶报告基因的抑制作用,IC50值为8.2 μM。在用10 ng/mL TNF-α处理后的HepG2细胞中,Ginsenoside Rb3 还以剂量依赖性的方式抑制 cyclooxygenase-2 (COX-2)inducible nitric oxide synthase (iNOS) 信使mRNA的诱导诱导表达。

S0924New

Pteryxin

Pteryxin ((+)-Pteryxin) 是一种在 Apiaceae 伞形科中发现的二氢吡喃香豆素衍生物,也是一种有效的 butyrylcholinesterase (BChE) 的抑制剂,IC50值为12.96 μg/ml。Pteryxin 可抑制LPS诱导的小鼠腹膜巨噬细胞中 nitric oxide 的产生,其IC50值为20 μM。Pteryxin 具有治疗阿尔茨海默氏病 (AD) 的潜力。

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)

S8337

1400W 2HCl

1400W (N-(3-(Aminomethyl)benzyl)acetamidine) 是iNOS的抑制剂,与iNOS缓慢、紧密地结合,具有选择性。

S3261New

Myrislignan

Myrislignan 是一种分离自Myristica fragrans Houtt的木脂素并具有抗炎活性。Myrislignan 可抑制 interleukin-6 (IL-6)tumour necrosis factor-α (TNF-α)。Myrislignan 剂量依赖性地抑制LPS刺激的巨噬细胞中 inducible NO synthase (iNOS)cyclooxygenase-2 (COX-2) 的表达。Myrislignan 可抑制 NF-κB 信号通路的激活。

S3304New

Stylopine

Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) 可降低LPS刺激引起的 nitric oxide (NO)prostaglandin E2 (PGE2)tumor necrosis factor-alpha (TNF-alpha)interleukin-1beta (IL-1beta)IL-6 的生成,以及 cyclooxygenase-2 (COX-2) 的活性。Stylopine 是 Chelidonium majus L 的叶子的主要成分。

S6850New

NE 52-QQ57

NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂,其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累,在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加,包括 tumor necrosis factor-α (TNF-α)interleukin (IL)-1βIL-6inducible nitric oxide synthase (iNOS)nitric oxide (NO)cyclooxygenase 2 (COX2)prostaglandin E2 (PGE2)

S3292New

Falcarindiol

Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) 是一种天然的聚乙炔化合物,存在于伞形科的许多植物中。Falcarindiol 可抑制LPS刺激的 inducible nitric oxide synthase (iNOS)tumor necrosis factor alpha (TNFα)interleukin-6 (IL-6)interleukin-1 beta (IL-1β) 的表达。Falcarindiol 可减弱LPS诱导的 JNKERKSTAT1STAT3 信号分子的激活。

S4962

Agmatine sulfate

Agmatine sulfate是精氨酸的活性代谢产物,能够提高一氧化氮水平、减少血糖水平并提高生长激素水平。

S9029

Prim-o-glucosylcimifugin

Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) 是防风(Radix Saposhnikovia)中的主要成分,长期以来一直应用于传统中医药中治疗发热、风湿和癌症,它表现出潜在的抗癌活性。在LPS激活的 RAW 264.7 巨噬细胞,Prim-O-glucosylcimifugin 可以浓度依赖性的方式下调 NO synthase (iNOS)cyclooxygenase 2 (COX-2) 的mRNA和蛋白质表达。

S3931

Ginsenoside Rd

Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.

S9374

2',5'-Dihydroxyacetophenone

2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) 是二羟基苯乙酮异构体的混合物,用于食品调味。2',5'-Dihydroxyacetophenone 通过抑制 iNOS 的表达来显着抑制 NO 的产生。2',5'-Dihydroxyacetophenone 可通过阻断 ERK1/2NF-κB 信号通路来显著地降低促炎细胞因子 TNF-αIL-6 的表达水平。

S3899

Hederagenin

Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB.

S9502

Madecassic acid

Madecassic acid (Brahmic acid) 是最早从积雪草中分离的天然三萜,具有多种消炎和抗糖尿病作用,阻断巨噬细胞中的 NF-κB 活化并导致 iNOSCOX-2TNF-alphaIL-1betaIL-6 抑制。

S4548

Aminoguanidine hydrochloride

Aminoguanidine (Pimagedine, Guanyl hydrazine, Hydrazinecarboximidamide, Imino semicarbazide, Monoaminoguanidine)是二胺氧化酶一氧化氮合成酶抑制剂。它通过与3-deoxyglucosone相互作用减少晚期糖基化终末产物(AGEs)水平。

S3924

Ginsenoside Rb1

Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.

S5542

7-Nitroindazole

7-Nitroindazole, a heterocyclic compound, acts as a selective inhibitor for neuronal nitric oxide synthase showing a 10-fold selectivity for neuronal NOS.

S5229

Isosorbide dinitrate

Isosorbide Dinitrate (ISDN, Sorbide nitrate, Sorbidnitrate, Isordil, Nitrosorbide)是异山梨醇(isosorbide)的二硝酸盐形式,这是一种具有血管扩张活性的有机硝酸盐。Isosorbide Dinitrate 是一种用于心力衰竭、食道痉挛的药物,用于治疗和预防因没有足够的血液流向心脏而引起的胸痛。Isosorbide Dinitrate 可转化为一氧化氮(NO),一种活性中间化合物,可激活 the enzyme guanylate cyclase (atrial natriuretic peptide receptor A)

S6962New

TPEN

TPEN (TPEDA) 是一种可透过细胞的重金属螯合剂,可通过负调控细胞内 NOZn2+ 信号转导来诱导NB4细胞凋亡。TPEN(TPEDA)可能是APL (acute promyelocytic leukemia) 的潜在治疗策略之一。

S5577

6-Biopterin

6-Biopterin ( L-Biopterin, L-Erythro-Biopterin) is a natural product that has been considered as a growth factor for some insects.

S3174

L-Arginine HCl (L-Arg)

L-Arginine HCl (L-Arg)是一氧化氮合成的氮供体,是一种有效的血管舒张药,在镰状细胞性贫血时含量不足。

目录号 产品描述 文献引用 实验数据
S2877

L-NAME HCl

L-NAME HCl是一种无选择性的一氧化氮合成酶抑制剂,对nNOS (牛源), eNOS (人源)和iNOS (鼠源)的Ki值分别为15nM, 39 nM和4.4 μM。

S9208

Ginsenoside Rb3

Ginsenoside Rb3 是从人参中提取的天然产物,在心血管疾病包括心肌的缺血/再灌注(I/R)损伤中起着重要作用。在人肾293T细胞中检测了Ginsenoside Rb3(0.1-10 μM)对肿瘤坏死因子TNF-α诱导的 nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) 荧光素酶报告基因的抑制作用,IC50值为8.2 μM。在用10 ng/mL TNF-α处理后的HepG2细胞中,Ginsenoside Rb3 还以剂量依赖性的方式抑制 cyclooxygenase-2 (COX-2)inducible nitric oxide synthase (iNOS) 信使mRNA的诱导诱导表达。

S0924New

Pteryxin

Pteryxin ((+)-Pteryxin) 是一种在 Apiaceae 伞形科中发现的二氢吡喃香豆素衍生物,也是一种有效的 butyrylcholinesterase (BChE) 的抑制剂,IC50值为12.96 μg/ml。Pteryxin 可抑制LPS诱导的小鼠腹膜巨噬细胞中 nitric oxide 的产生,其IC50值为20 μM。Pteryxin 具有治疗阿尔茨海默氏病 (AD) 的潜力。

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)

S8337

1400W 2HCl

1400W (N-(3-(Aminomethyl)benzyl)acetamidine) 是iNOS的抑制剂,与iNOS缓慢、紧密地结合,具有选择性。

S3261New

Myrislignan

Myrislignan 是一种分离自Myristica fragrans Houtt的木脂素并具有抗炎活性。Myrislignan 可抑制 interleukin-6 (IL-6)tumour necrosis factor-α (TNF-α)。Myrislignan 剂量依赖性地抑制LPS刺激的巨噬细胞中 inducible NO synthase (iNOS)cyclooxygenase-2 (COX-2) 的表达。Myrislignan 可抑制 NF-κB 信号通路的激活。

S3304New

Stylopine

Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) 可降低LPS刺激引起的 nitric oxide (NO)prostaglandin E2 (PGE2)tumor necrosis factor-alpha (TNF-alpha)interleukin-1beta (IL-1beta)IL-6 的生成,以及 cyclooxygenase-2 (COX-2) 的活性。Stylopine 是 Chelidonium majus L 的叶子的主要成分。

S6850New

NE 52-QQ57

NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂,其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累,在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加,包括 tumor necrosis factor-α (TNF-α)interleukin (IL)-1βIL-6inducible nitric oxide synthase (iNOS)nitric oxide (NO)cyclooxygenase 2 (COX2)prostaglandin E2 (PGE2)

S3292New

Falcarindiol

Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) 是一种天然的聚乙炔化合物,存在于伞形科的许多植物中。Falcarindiol 可抑制LPS刺激的 inducible nitric oxide synthase (iNOS)tumor necrosis factor alpha (TNFα)interleukin-6 (IL-6)interleukin-1 beta (IL-1β) 的表达。Falcarindiol 可减弱LPS诱导的 JNKERKSTAT1STAT3 信号分子的激活。

S4962

Agmatine sulfate

Agmatine sulfate是精氨酸的活性代谢产物,能够提高一氧化氮水平、减少血糖水平并提高生长激素水平。

S9029

Prim-o-glucosylcimifugin

Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) 是防风(Radix Saposhnikovia)中的主要成分,长期以来一直应用于传统中医药中治疗发热、风湿和癌症,它表现出潜在的抗癌活性。在LPS激活的 RAW 264.7 巨噬细胞,Prim-O-glucosylcimifugin 可以浓度依赖性的方式下调 NO synthase (iNOS)cyclooxygenase 2 (COX-2) 的mRNA和蛋白质表达。

S3931

Ginsenoside Rd

Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.

S9374

2',5'-Dihydroxyacetophenone

2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) 是二羟基苯乙酮异构体的混合物,用于食品调味。2',5'-Dihydroxyacetophenone 通过抑制 iNOS 的表达来显着抑制 NO 的产生。2',5'-Dihydroxyacetophenone 可通过阻断 ERK1/2NF-κB 信号通路来显著地降低促炎细胞因子 TNF-αIL-6 的表达水平。

S3899

Hederagenin

Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB.

S9502

Madecassic acid

Madecassic acid (Brahmic acid) 是最早从积雪草中分离的天然三萜,具有多种消炎和抗糖尿病作用,阻断巨噬细胞中的 NF-κB 活化并导致 iNOSCOX-2TNF-alphaIL-1betaIL-6 抑制。

S4548

Aminoguanidine hydrochloride

Aminoguanidine (Pimagedine, Guanyl hydrazine, Hydrazinecarboximidamide, Imino semicarbazide, Monoaminoguanidine)是二胺氧化酶一氧化氮合成酶抑制剂。它通过与3-deoxyglucosone相互作用减少晚期糖基化终末产物(AGEs)水平。

S3924

Ginsenoside Rb1

Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.

S5542

7-Nitroindazole

7-Nitroindazole, a heterocyclic compound, acts as a selective inhibitor for neuronal nitric oxide synthase showing a 10-fold selectivity for neuronal NOS.

目录号 产品描述 文献引用 实验数据
S5229

Isosorbide dinitrate

Isosorbide Dinitrate (ISDN, Sorbide nitrate, Sorbidnitrate, Isordil, Nitrosorbide)是异山梨醇(isosorbide)的二硝酸盐形式,这是一种具有血管扩张活性的有机硝酸盐。Isosorbide Dinitrate 是一种用于心力衰竭、食道痉挛的药物,用于治疗和预防因没有足够的血液流向心脏而引起的胸痛。Isosorbide Dinitrate 可转化为一氧化氮(NO),一种活性中间化合物,可激活 the enzyme guanylate cyclase (atrial natriuretic peptide receptor A)

目录号 产品描述 文献引用 实验数据
S6962New

TPEN

TPEN (TPEDA) 是一种可透过细胞的重金属螯合剂,可通过负调控细胞内 NOZn2+ 信号转导来诱导NB4细胞凋亡。TPEN(TPEDA)可能是APL (acute promyelocytic leukemia) 的潜在治疗策略之一。

目录号 产品描述 文献引用 实验数据
S5577

6-Biopterin

6-Biopterin ( L-Biopterin, L-Erythro-Biopterin) is a natural product that has been considered as a growth factor for some insects.

S3174

L-Arginine HCl (L-Arg)

L-Arginine HCl (L-Arg)是一氧化氮合成的氮供体,是一种有效的血管舒张药,在镰状细胞性贫血时含量不足。