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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1787 |
Levobupivacaine
|
Sodium Channel | Membrane transporter/Ion channel |
Levobupivacaine 是一种氨基酰胺类局麻药,属于n-alkylsubstituted pipecoloxylidide 家族。它是bupivacaine 的 S-对映异构体。 | |||
T22394 |
Paritaprevir
ABT450,ABT-450,帕利普韦,Veruprevir |
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
Paritaprevir (ABT450) 是一种非结构蛋白 3/4A 蛋白酶抑制剂,对 HCV 1a 和 HCV 1b 的 EC50 值分别为 1 和 0.21 nM。它也是SARS-CoV 3CLpro 的抑制剂,IC50为 1.31 μM。 | |||
T6566 |
Levobupivacaine hydrochloride
Levobupivacaine HCl,(S)-(-)-Bupivacaine HCl,盐酸左布比卡因,(S)-(-)-Bupivacaine monohydrochloride |
Sodium Channel | Membrane transporter/Ion channel |
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是有效的钠通道阻滞剂。 | |||
T22003 |
2,3-dihydrothieno-Thiadiazole Carboxylate
|
P450 | Metabolism |
2,3-dihydrothieno-Thiadiazole Carboxylate 是一种 CYP450(CYP2E1 和 CYP2B4)抑制剂。 | |||
T20373 |
1-Phenylpyrrole
NSC16581,NSC-16581,1-苯基吡咯,NSC 16581 |
Others | Others |
1-Phenylpyrrole (NSC-16581) 可抑制大鼠肝脏微粒体中 CYP450 依赖性单加氧酶活性。 | |||
T4983 |
Isoetharine mesylate salt
Isoetarine mesilate,异丙肾上腺素甲磺酸盐 |
Others; Adrenergic Receptor | GPCR/G Protein; Neuroscience; Others |
Isoetharine mesylate salt (Isoetarine mesilate) 是一种 β-肾上腺素能受体激动剂。它还是能够上调 CYP450 表达的孕烷 X 受体(PXR) 激活剂。 | |||
T37826 |
CAY10462
CAY10462,CTK8E8405 |
P450 | Metabolism |
CAY10462 (CTK8E8405) 是一种有效的 20-HETE 合酶 CYP4A11 的选择性抑制剂,IC50 为 8.8 nM。 CAY10462 对 1A、1C 和 3A CYP450 酶的效力降低近 200 倍。 | |||
T4567 |
Sulfaphenazole
Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide |
P450; Antibacterial | Metabolism; Microbiology/Virology |
Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂,抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应,增加 AP-1的氧化应激和激活。 | |||
T1540 |
Doxepin hydrochloride
Toruan,Doxepin HCl,Aponal,Novoxapin,盐酸多塞平 |
P450; Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience |
Doxepin hydrochloride (Aponal) 是一种可口服的三环抗抑郁剂,是选择性组胺受体 H1拮抗剂。它也是 CYP450抑制剂,抑制 CYP450 2C19和 CYP450 1A2。 | |||
T11556 |
HET0016
|
Others | Others |
HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis). HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angi | |||
T11847L |
Liarozole
R75251 dihydrochloride,利阿唑 |
P450; Retinoid Receptor | Metabolism |
Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物,是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA),具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM),导致组织维甲酸水平增加。 | |||
T14186 |
17-ODYA
17-十八炔酸,Alkynyl Stearic Acid |
Others; PROTAC Linker | Others; PROTAC |
Alkynyl Stearic Acid 是 CYP450 ω-羟化酶抑制剂。它能够抑制与花生四烯酸孵育的大鼠肾皮质微粒体形成 20-HETE 、dihydroxyeicosatrienoic acids、epoxyeicosatrienoic acids。它可以改善异丙肾上腺素诱导的培养心肌细胞凋亡和坏死。 | |||
T14841 |
BVT948
|
Phosphatase; P450; Histone Methyltransferase | Chromatin/Epigenetic; Metabolism |
BVT948 是一种蛋白酪氨酸磷酸酶抑制剂,还可以抑制赖氨酸甲基转移酶 SETD8 (KMT5A) 和几种细胞色素 P450 (P450) 同工型。 | |||
T16704 |
Quilseconazole
VT-1129 |
Others | Others |
Quilseconazole is an effective, orally active fungal Cyp51 inhibitor. it also binds tightly to cryptococcal CYP51 but weakly inhibits humans CYP450 enzymes. | |||
T37180 |
Avanafil metabolite M16
|
Others | Others |
Avanafil metabolite M16 is a major inactive metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M16 and avanafil metabolite M4 , as well as minor metabolites. | |||
T25716L |
Liarozole HCl
R75251,Liarozole hydrochloride,R 75251,R-75251 |
Others | Others |
Liarozole HCl is a benzimidazole derivative with antineoplastic activity. As a retinoic acid metabolism blocking agent, liarozole inhibits CYP450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, leading to an increase in endogenous ATRA production, | |||
T78154 |
CS640
|
Others | Others |
CS640是一种钙调蛋白依赖性激酶选择性抑制剂,对CaMK1D、CaMK1B、CaMK1A、CaMK1G、PIP5K1C、MEK5、RIPK4和MLK3的抑制作用的IC50值分别为0.08、0.03、0.001、0.001、11.2、0.025、5.69和2.75μM。此外,CS640对CYP450 2C9和CYP450 2C19的IC50值分别为6和10μM。 | |||
T37181 |
Avanafil metabolite M4
Avanafil metabolite M4 |
Others | Others |
Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16 , as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil. | |||
T35847 |
16(R)-HETE
|
Others | Others |
Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that... | |||
T37234 |
(±)14(15)-EpETE
|
Others | Others |
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids, produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoi... | |||
T37238 |
(±)19(20)-EpDPA
|
Others | Others |
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic... | |||
T37235 |
(±)16(17)-EpDPA
(±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA |
Others | Others |
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators.[1],[2]Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EET which are prime candidates for the actual active mediator.[3] However, the CYP450 metabolites of eicosapentaenoic acid and docosahex... | |||
T11847 |
Liarozole dihydrochloride
R75251 dihydrochloride |
Others | Others |
Liarozole dihydrochloride is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders. | |||
T37788 |
Resorufin benzyl ether
|
||
Resorufin benzyl ether is a fluorometric probe that acts as a substrate for cytochrome P450 (CYP)3A4. It is typically used near its apparent Km value of 30 μM to screen the inhibition/activation potential of test compounds, to predict potential drug-drug interactions, or to monitor other CYP450 activities. Upon enzyme cleavage, resorufin benzyl ether generates a red fluorescent product (ex. 571 nm/em. 585 nm). | |||
T36145 |
12(R)-HETE
|
Others | Others |
Biosynthesis of 12(R)-HETE in invertebrates is via lipoxygenation of arachidonic acid . In mammals, 12(R)-HETE can be produced by 12(R)-LOs and also by CYP450 oxidation. The activity of 12(R)-HETE in mammals is predominantly proinflammatory. 12(R)-HETE exhibits dose-dependent leukocyte chemotaxis at concentrations as low as 100 nM, and lowers intraocular pressure in rabbits. | |||
T35848 |
16(S)-HETE
|
Others | Others |
Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 μM. | |||
T35467 |
(±)18-HETE
|
Others | Others |
(±)18-HETE is the racemic version of a cytochrome P450 (CYP450) metabolite of arachidonic acid. When formed by the CYP2E1 isoform, 18-HETE is comprised 100% of the (R) isomer. 18(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, whereas 18(S)-HETE does not affect perfusion pressure. 18-HETE has negligible effects on ATPase activity. 18(R)-HETE at 1 μM completely blocks 20-HETE-induced vasoconstriction of renal arterioles. | |||
T37241 |
(±)4(5)-EpDPA methyl ester
|
Others | Others |
(±)4(5)-EpDPA methyl ester is a derivative of (±)4(5)-EpDPA which is stable enough to ship and handle routinely. The active free acid can be regenerated from the methyl ester by careful base hydrolysis. (±)4(5)EpDPA is a CYP450 metabolite of DHA which can be further metabolized to the diol metabolite. There are no published reports on the biological activity of (±)4(5)-EpDPA methyl ester at this time. | |||
T35523 |
(±)17-HETE
|
Others | Others |
Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)17-HETE is the racemic version of a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney. At a concentration of 2 μM the (S)-enantiomer of 17-HETE inhibits proximal tubule ATPase activity by as much as 70%, whereas the (R)-isomer is inactive. | |||
T37228 |
(±)8(9)-EpETE
|
Others | Others |
Eicosapentaenoic acid is converted to epoxyeicosatetraenoic acids (EpETEs) by several cytochrome P450 isoforms. The major product of this epoxygenase pathway, (±)17(18)-EpETE , relaxes vascular and airway smooth muscle by activating large conductance Ca2+-activated K+ (BKCa) channels by directly interacting with BKα channel subunits. (±)8(9)-EpETE is an epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo. The biological actions and physiological effects of this epox... | |||
T35849 |
17(S)-HETE
|
Others | Others |
Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites.17-HETE is a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney.17(S)-HETE inhibits proximal tubule ATPase activity by as much as 70% at a concentration of 2 μM. | |||
T35850 |
19(S)-HETE
|
Others | Others |
19-HETE is one of the major cytochrome P450 (CYP450) metabolites of arachidonic acid that is released from the kidney in response to angiotensin II. When formed by the CYP2E1 isoform, 19-HETE is composed of 70% and 30% of the (S) and (R) stereoisomers, respectively. Both 19(S)- and 19(R)-HETE are potent vasodilators of renal preglomerular vessels. 19(S)-HETE stimulates both renal sodium-potassium ATPase and volume absorption in the rabbit proximal straight tubule. | |||
T37708 |
17(R)-HETE
|
Others | Others |
Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 17-HETE is a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney. 17(R)-HETE is an inactive isomer of 17-HETE, whereas the (S) enantiomer can inhibit proximal tubule ATPase activity at a concentration of 2 μM. | |||
T36216 |
19(R)-HETE
|
Others | Others |
19-HETE is one of the major cytochrome P450 (CYP450) metabolites of arachidonic acid that is released from the kidney in response to angiotensin II. When formed by the CYP2E1 isoform, 19-HETE is composed of 70% and 30% of the (S) and (R) stereoisomers, respectively. Both 19(S)- and 19(R)-HETE are potent vasodilators of renal preglomerular vessels. However, 19(R)-HETE at 1 μM completely blocks 20-HETE-induced vasoconstriction of renal arterioles, whereas 19(S)-HETE remains inactive. | |||
T84501 |
(±)11(12)-EpETE
(±)11,12-EEQ |
Others | Others |
Eicosapentaenoic acid (EPA) is metabolized into epoxyeicosatetraenoic acids (EpETE) by multiple cytochrome P450 isoforms. The predominant compound of this epoxygenase pathway, (±)17(18)-EpETE, induces relaxation in vascular and airway smooth muscles through its action on large conductance Ca2+-activated K+ (BKCa) channels, specifically by binding to the BKα channel subunits. Another notable epoxygenase pathway derivative, (±)11(12)-EpETE, also generated from EPA via CYP450 activity in both in vi... | |||
T73898 |
Paritaprevir dihydrate
|
Others | Others |
Paritaprevir (ABT-450) dihydrate,一种口服非结构蛋白3/4A (NS3/4A) 蛋白酶抑制剂,对HCV1a 和 1b 具有高效抗病毒活性,EC50值分别为1 nM 和 0.21 nM。此外,其作为SARS-CoV3CLpro 抑制剂,IC50为1.31 μM。其主要通过细胞色素P450 (CYP) 3A代谢,且利托那韦 (Ritonavir,CYP450 抑制剂) 能增强其血浆浓度和延长半衰期。 | |||
T35465 |
(±)16-HETE
|
Others | Others |
Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)16-HETE is the racemic version of a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation. The biological activity of 16-HETE is stereospecific. 16(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, however 16(S)-HETE does not affect perfusion pressure. At a concentration of 2 μM the (S)-enantiomer of 16-HETE inhibits pro... | |||
T35715 |
N-desmethyl Eletriptan
|
Others | Others |
N-desmethyl Eletriptan is a metabolite of eletriptan .1It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes. 1.Evans, D.C., O’Connor, D., Lake, B.G., et al.Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoproteinDrug Metab. Dispos.31(7)861-869(2003) | |||
T35494 |
(±)11(12)-EET
|
Others | Others |
(±)11(12)-EET is a fully racemic version of the R/S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in t... | |||
T79568 |
NPD-2975
|
Parasite | Microbiology/Virology |
NPD-2975(化合物30)是一款口服活性的抗锥虫药物,用于治疗非洲人类锥虫病(HAT)。在MRC-5人肺成纤维细胞及T. b. brucei感染的小鼠模型中,NPD-2975毒性低。此化合物展现了良好的代谢稳定性,在体外对T. b. brucei IC500抑制浓度为70 nM。NPD-2975还可抑制CYP450酶,对CYP1A2和CYP2C19的IC50分别为0.16 μM和0.42 μM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2S0663 |
Humantenmine
|
P450 | Metabolism |
Humantenmine 是一种分离自中国线虫中的生物碱,有用于疼痛和风湿性关节炎的研究潜力。 | |||
T3696 |
polygalaxanthone III
|
Others; P450 | Metabolism; Others |
Polygalaxanthone III 提取自远志polygala tenuifolia wild,可抑制CYP450酶。它能够抑制由 CYP2E1 催化的氯唑沙宗 6-羟基化(IC50:50.56μM)。 | |||
T5786 |
TETRAHYDROPIPERINE
四氢胡椒碱,Cosmoperine |
P450; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
Tetrahydropiperine (Cosmoperine) 是胡椒碱的环己基类似物,也是一种天然芳基戊酰胺,从Piper longum 分离得到。它对细胞色素 P450 (CYP) 同工型 CYP1A1/芳基烃羟化酶 (AHH;IC50=23 µM)具有抑制作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11088 |
Doxepin D3 Hydrochloride
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Doxepin D3 Hydrochloride is a deuterium-labeled doxepin hydrochloride.Doxepin hydrochloride is an oral active tricyclic antidepressant used as a sedative.Doxepin hydrochloride is also an effective CYP450 inhibitor, significantly inhibiting CYP450 2C19 and |