45
10
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T63496 | CYP2C9/CYP2C19-IN-1 | ||
CYP2C9/CYP2C19-IN-1 是无肝脏毒性和遗传毒性的CYP2C9/CYP2C19强效抑制剂,能够用于研究寨卡病毒 (ZIKV) 感染。 | |||
T25283 |
Cytochrome P450 2C9
Cyp2C9,Human cytochrome P450 2C9,Cytochrome P 450 2C9,S-Mephenytoin 4-hydroxylase |
||
Cytochrome P450 2C9 is a cytochrome P-450 subtype that possesses specificity for acidic xenobiotics. It oxidizes a wide range of important clinical drugs under the categories of nonsteroidal anti-inflammatory agents, anticoagulants, hypoglycemic agents, a | |||
T10423 |
AWZ1066S
|
Parasite | Microbiology/Virology |
AWZ1066S 是一种高度特异性抗Wolbachia 的候选药物,可短期研究丝虫病,其在细胞中测得的EC50值为 2.5 nM。 | |||
T2088 |
APD668
APD 668 |
GPR; P450; Potassium Channel | Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
APD668 是选择性的,口服有效的GPR119激动剂,对hGPR119和rGPR119的EC50分别为 2.7 nM 和 33 nM。它对除CYP2C9(Ki=0.1 μM) 以外的五种主要 CYP 亚型均无明显抑制作用。它可用于脂肪性肝炎和糖尿病的研究。 | |||
T3610 |
Ranitidine
雷尼替丁,HSDB 3925,Ranitidin |
P450; Antibacterial; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience |
Ranitidine (HSDB 3925) 是一种选择性的,具有口服活性的组胺 H2 受体拮抗剂,IC50为 3.3 μM。它还一种是CYP2C19和CYP2C9的弱抑制剂,可抑制胃液分泌。 | |||
T0865 |
Ranitidine Hydrochloride
AH19065,盐酸雷尼替丁 |
P450; Antibacterial; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience |
Ranitidine Hydrochloride (AH19065) 是一种具有口服活性的组胺 H2 受体选择性拮抗剂,IC50为 3.3 μM。它还是一种CYP2C19和CYP2C9的弱抑制剂,可抑制胃液分泌。 | |||
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。 | |||
T1274 |
Benzbromarone
Desuric,Normurat,苯溴马隆,Urinorm |
Apoptosis; P450; Xanthine Oxidase | Apoptosis; Metabolism |
Benzbromarone (Desuric) 是一种高效的,耐受性良好的非竞争性黄嘌呤氧化酶抑制剂,用作排尿酸剂,研究痛风。 | |||
T10632 |
Bucolome
Paramidin,5-Butyl-1-cyclohexylbarbituric acid,Paramidine,Bucolom,布可隆,Bucolomum |
P450; Immunology/Inflammation related | Immunology/Inflammation; Metabolism |
Bucolome (Paramidine) 是一种 CYP2C9 抑制剂,具有排尿酸和抗炎活性。 | |||
T72617 |
Nampt activator-2
|
P450; NAMPT | Metabolism |
Nampt activator-2 是一种 NAMPT 激活剂(EC50 : 0.023 μM)。 Nampt activator-2 对 CYP2C9、2D6、2C19 具有亲和力,亲和力数值分别为 0.060 μM、 0.41 μM 和 0.59 μM 。Nampt activator-2 可用来研究动脉粥样硬化,肥胖,II型糖尿病,胰岛素抵抗和I型糖尿病。 | |||
T41291 |
MS-PPOH
|
P450 | Metabolism |
MS-PPOH 是一种有效的选择性细胞色素 P450 (CYP) 环氧化酶抑制剂。MS-PPOH 抑制 CYP2C8 和 CYP2C9,IC50 分别为 15 和 11 µM。 | |||
T2753 |
Avasimibe
PD-148515,阿伐麦布,CI-1011 |
P450; Acyltransferase | Metabolism |
Avasimibe (PD-148515) 是一种口服有效的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂,对 ACAT1和 ACAT2的 IC50分别为 24 和 9.2 µM。Avasimibe 在前列腺癌中有研究的价值。 | |||
T77517 |
URAT1 inhibitor 7
|
OAT | Membrane transporter/Ion channel |
URAT1 inhibitor 7 是一种新型高效的人尿酸转运蛋白 URAT1 抑制剂 (IC50:12 nM)。URAT1 inhibitor 7 对 CYP2C9 具有抑制作用,IC50为4.2 μM。URAT1 inhibitor 7 可用于研究高尿酸血症和痛风。 | |||
T4190 |
Ticlopidine
PCR 5332,Ticlid,噻氯匹定 |
ATPase; Adiponectin receptor | GPCR/G Protein; Membrane transporter/Ion channel |
Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂,抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂,能够阻断 NTPDase 同工酶,对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。 | |||
T1149 |
Fenofibrate
Procetofen,非诺贝特,Lipanthyl,Lipantil |
P450; PPAR; Autophagy | Autophagy; DNA Damage/DNA Repair; Metabolism |
Fenofibrate (Lipanthyl) 是一种选择性PPARα激动剂,EC50为 30 μM。它是一种合成的苯氧基异丁酸衍生物和前药,具有抗高血脂活性。它抑制细胞色素 P450 亚型, 对CYP2C19、CYP2B6、CYP2C9、CYP2C8和CYP3A4的IC50分别为 0.2、0.7、9.7、4.8 和 142.1 μM。 | |||
T4488 |
GSK-25
GSK25 |
ROCK; S6 Kinase; mTOR | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
GSK-25 是一种选择性的,具有口服活性的 ROCK1抑制剂。它对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性,RSK1的 IC50 为 398 nM,p70S6K 的 IC50 为 1000nM。它可抑制 P450,对 CYP2C9、CYP2D6和 CYP3A4的 IC50分别为2.5、5.2和2.5 μM。 | |||
T1415 |
Gemfibrozil
吉非罗齐,CI-719,Jezil,Decrelip,Lopid |
P450; Adrenergic Receptor; PPAR | DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience |
Gemfibrozil (CI-719) 是一种PPAR-α激活剂,可作为降脂药。它也是P450非选择性抑制剂,对 CYP2C9、2C19、2C8 和 1A2 的Ki 值分别为 5.8、24、69 和 82 μM。 | |||
T35530 |
IHMT-PI3Kδ-372
IHMT-PI3Kδ-372 |
PI3K | PI3K/Akt/mTOR signaling |
IHMT-PI3Kδ-372 是一种选择性的 PI3Kδ 抑制剂,IC50 为 14 nM,可用于慢性阻塞性肺病的研究。 | |||
T11584 |
Hydroxy desmethyl Bosentan
Ro 64-1056 |
Others | Others |
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. | |||
T13135 |
Tetrahydrocurcumin D6
HZIV 81-2 D6 |
Others | Others |
Tetrahydrocurcumin D6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin displays inhibitory activity for CYP2C9 and CYP3A4. | |||
T38911 |
Nav1.7-IN-8
Nav1.7-IN-8 |
||
Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain. | |||
T63495 | CYP2C1/CYP2C19-IN-2 | ||
CYP2C1/CYP2C19-IN-2 是无肝脏毒性和遗传毒性的CYP2C9/CYP2C19强效抑制剂,能够用于研究寨卡病毒 (ZIKV) 感染。 | |||
T36769 |
10-hydroxy Warfarin
|
||
10-hydroxy Warfarin is a metabolite of (R)-warfarin .1It is formed from (R)-warfarin by the cytochrome P450 (CYP) isoform CYP3A4. 10-hydroxy Warfarin is an inhibitor of CYP2C9 (IC50= 1.6 μM), the enzyme that converts (S)-warfarin to its 6-hydroxy warfarin and 7-hydroxy warfarin metabolites.2 1.Kaminsky, L.S., and Zhang, Z.-Y.Human P450 metabolism of warfarinPharmacol. Ther.73(1)67-74(1997) 2.Jones, D.R., Kim, S.-Y., Guderyon, M., et al.Hydroxywarfarin metabolites potently inhibit CYP2C9 metaboli... | |||
T35640 |
trans-carboxy Glimepiride
|
||
trans-carboxy Glimepiride is a metabolite of the sulfonylurea glimepiride .1It is formed from glimepiride in a two-step process mediated by the cytochrome P450 (CYP) isoform CYP2C9 and cytosolic enzymes. 1.Noh, K., Kim, E., Jeong, T.C., et al.Simultaneous determination of glimepiride and its metabolites in human plasma by liquid chromatography coupled to a tandem mass spectrometryArch. Pharm. Res.34(12)2073-2078(2011) | |||
T70786 |
ML252
|
||
ML252是一种钾离子通道(potassium channel)的选择性抑制剂,主要针对KCNQ2 (Kv7.2,IC50=69 nM)。同时,ML252对细胞色素Cytochrome P450也有抑制作用,其IC50值分别为CYP1A2为6.1 nM、CYP2C9为18.9 nM、CYP3A4为3.9 nM、CYP2D6为19.9 nM。 | |||
T36187 |
Celecoxib Carboxylic Acid
|
||
Celecoxib carboxylic acid is an inactive metabolite of the COX-2 inhibitor celecoxib .1,2It is formed from celecoxib primarily by the cytochrome P450 (CYP) isoform CYP2C9. 1.Liu, H., Huang, X., Shen, J., et al.Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: Molecular docking and 3D QSAR analysesJ. Med. Chem.45(22)4816-4827(2002) 2.Kim, S.-H., Kim, D.-H., Byeon, J.-Y., et al.Effects of CYP2C9 genetic polymorphisms on the pharmacokinetics of celecox... | |||
T35641 |
trans-hydroxy Glimepiride
|
||
trans-hydroxy Glimepiride is an active metabolite of the sulfonylurea glimepiride .1It is formed from glimepiride primarily in the liver by the cytochrome P450 (CYP) isoform CYP2C9. 1.Langtry, H.D., and Balfour, J.A.Glimepiride. A review of its use in the management of type 2 diabetes mellitusDrugs55(4)563-584(1998) | |||
T11187 | EMT inhibitor-2 | Others | Others |
EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively. EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. | |||
T78590 |
Dibenzylfluorescein
DBF |
||
Dibenzylfluorescein(DBF)是一款荧光探针,作为细胞色素P450(CYP)亚型,包括CYP3A4、CYP2C8、CYP2C9、CYP2C19和CYP19的特异性底物,常在Km值0.87-1.9 µM(Ex=485nm,Em=535nm)范围内应用。该探针主要用于监测药物或疾病导致的CYP催化活性变化。 | |||
T14040 |
4-Hydroxytolbutamide
Hydroxytolbutamide |
Potassium Channel | Membrane transporter/Ion channel |
4-Hydroxytolbutamide(Hydroxytolbutamide), a metabolite of Tolbutamide, which is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2]. | |||
T62825 | URAT1 inhibitor 2 | ||
URAT1 inhibitor 2 是一种口服具有活力的 URAT1 和 CYP isozyme 抑制剂,对 URAT1 介导的 14C-UA 吸收、CYP1A2、CYP2C9 的 IC50 值分别为 1.36 μM、16.97 μM、5.22 μM。URAT1 inhibitor 2 是一种有前途的、能够用于研究高尿酸血症和痛风的候选药物。 | |||
T78925 |
HIV-1 inhibitor-58
|
||
HIV-1inhibitor-58(Compound 10c)是一款抗逆转录病毒活性的广谱非核苷逆转录酶抑制剂,有效抑制MT-4细胞中的HIV-1 WT株IIIB以及NNRTI耐药菌株,如K103N和E138K(EC50 < 50 nM)。此外,HIV-1inhibitor-58对CYP2C9与CYP2C19也表现出抑制作用(IC50分别为2.06 μM与1.91 μM),适用于HIV感染研究。 | |||
TMIH-0110 |
Benzbromarone-d5
|
||
Benzbromarone-d5 是 Benzbromarone 的氘代化合物。Benzbromarone 的 CAS 号为 3562-84-3。Benzbromarone 是一种高效的,耐受性良好的非竞争性黄嘌呤氧化酶抑制剂,用作排尿酸剂,研究痛风。 | |||
T36561 |
(3S)-hydroxy Quinidine
|
||
(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-depe... | |||
T35718 |
N-desmethyl Rosuvastatin (sodium salt hydrate)
|
||
N-desmethyl Rosuvastatin is an active metabolite of the HMG-CoA reductase inhibitor rosuvastatin .1,2N-desmethyl Rosuvastatin is formed when rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.1 1.Macwan, J.S., Ionita, I.A., and Akhlaghi, F.A simple assay for the simultaneous determination of rosuvastatin acid, rosuvastatin-5S-lactone, and N-desmethyl rosuvastatin in human plasma using liquid chromatography-tand... | |||
T71302 |
Norfluoxetine-d5 HCl
|
||
Norfluoxetine-d5 is intended for use as an internal standard for the quantification of norfluoxetine by GC- or LC-MS. Norfluoxetine is an active metabolite of the antidepressant fluoxetine. It is formed from fluoxetine by the cytochrome P450 (CYP) isoforms CYP2C9, CYP2C19, and CYP3A. Norfluoxetine inhibits serotonin (5-HT) uptake in rat brain synaptosomal membrane preparations (Ki = 44.7 nM) and isolated human platelets (IC50 = ~15 nM). It has been found in the tissues of fish exposed to wastewa... | |||
T62452 | HIV-1 inhibitor-40 | ||
HIV-1 inhibitor-40 (Compound 4ab) 是一种 HIV-1 非核苷型逆转录酶抑制剂 (NNRTI) (EC50: 1.9 nM),体内没有明显急性毒性。HIV-1 inhibitor-40 对 CYP 的敏感性较低,作用于 CYP2C9 (IC50: 5.16 μM) 和 CYP2C19 (IC50: 4.51 μM)。 | |||
TMIH-0095 |
Apigenin-d4
|
||
Apigenin-d4 是 Apigenin 的氘代化合物。Apigenin 的 CAS 号为 520-36-5。Apigenin 是从韩信草中提取的一种天然产物,是一种竞争性CYP2C9抑制剂,Ki为 2 μM。它被用作镇静剂、温和的镇痛剂和安眠药。 | |||
TMIH-0096 |
Apigenin-d6
|
||
Apigenin-d6 是 Apigenin 的氘代化合物。Apigenin 的 CAS 号为 520-36-5。Apigenin 是从韩信草中提取的一种天然产物,是一种竞争性CYP2C9抑制剂,Ki为 2 μM。它被用作镇静剂、温和的镇痛剂和安眠药。 | |||
T7788 |
2-Phenyl-2-(1-piperidinyl)propane
|
Others | Others |
2-Phenyl-2-(1-piperidinyl)propane 是一种具有可逆性、选择性的人 CYP2B6抑制剂,其 IC50为 5.1 μM,Ki 为 5.6。它对 CYP2D6 、CYP3A 均有抑制作用,且 IC50值分别为74 μM、200 μM。 | |||
T35829 | CC-90005 | ||
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS... | |||
T10535L |
BI 653048 phosphate
|
P450 | Metabolism |
BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM). | |||
T10891 |
CRTH2-IN-1
Ramatroban analog |
P450 | Metabolism |
CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay. | |||
T10535 |
BI 653048
|
P450 | Metabolism |
BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor. | |||
T16097 |
MK-8318
|
Others | Others |
MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM). |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S1894 |
Linderane
|
P450 | Metabolism |
Linderane 分离自 Lindera strychnifolia,能够不可逆的抑制 cytochrome P450 2C9。它具有抗痉挛及缓解疼痛的功能。 | |||
T3417 |
Amentoflavone
Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin |
Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal | Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB |
Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物,有抗炎、抗氧化和神经保护等作用。 | |||
TQ0217 |
Gomisin G
戈米辛G,戈米辛 G |
P450; HIV Protease | Metabolism; Microbiology/Virology; Proteases/Proteasome |
Gomisin G 是一种有抗HIV 活性的天然产物。 | |||
T2878 |
Ginsenoside Rd
Panaxoside Rd,Sanchinoside Rd,人参皂苷Rd,人参皂苷 Rd,Gypenoside VIII |
P450; Calcium Channel; NF-κB; COX; Endogenous Metabolite | Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
Ginsenoside Rd (Gypenoside VIII) 抑制 TNFα 诱导的NF-κB 转录活性,还抑制COX-2和iNOSmRNA 的表达。它抑制CYP2D6、CYP1A2、CYP3A4和CYP2C9,也抑制Ca2+内流,有可能抑制或阻止肿瘤生长。 | |||
T3818 |
Fraxinol
|
Others; P450 | Metabolism; Others |
Fraxinol 是一种分离自半边莲中的化合物。 | |||
T3811 |
Ginsenoside C-K
20(S)-人参皂苷 C-K,Ginsenoside compound K,Ginsenoside K,人参皂苷 C-K |
P450; cell cycle arrest; COX; NO Synthase | Cell Cycle/Checkpoint; Immunology/Inflammation; Metabolism; Neuroscience |
Ginsenoside C-K (Ginsenoside K) 是 Ginsenoside Rb1 的细菌代谢物,可通过抑制诱生型一氧化氮合酶和COX-2来发挥抗炎作用。它在人肝微粒体中抑制CYP2C9和CYP2A6活性,IC50分别为 32.0±3.6 和 63.6±4.2 μM。 | |||
T5S2360 |
Corydaline
Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline |
P450; Virus Protease; Opioid Receptor; AChE | Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience |
Corydaline (Corydalin) 是从 Corydalis yanhusuo 提取的一种异喹啉生物碱,是一种新型促动力植物药的主要活性成分之一。它促进胃排空和小肠转运,促进胃的调节,具有抗乙酰胆碱酯酶、抗过敏和镇痛活性。 | |||
T2175 |
Apigenin
C.I. Natural Yellow 1,4',5,7-Trihydroxyflavone,NSC 83244,金银花,Apigenol,芹菜素,LY 080400 |
P450; Autophagy | Autophagy; Metabolism |
Apigenin (NSC 83244) 是从韩信草中提取的一种天然产物,是一种竞争性CYP2C9抑制剂,Ki 为 2 μM。它被用作镇静剂、温和的镇痛剂和安眠药。 | |||
T3662 |
Eleutheroside E
|
NF-κB | NF-κB |
Eleutheroside E 是刺五加的重要成分,具有抗炎,保护缺血心脏的功能。 | |||
T3735 |
Tetrahydrocurcumin
Sabiwhite,Tetrahydrodiferuloylmethane,四氢姜黄素,HZIV 81-2,Tetrahydro Curcumin |
P450; Endogenous Metabolite; Autophagy | Autophagy; Metabolism |
Tetrahydrocurcumin (HZIV 81-2) 是从姜黄中发现的一种天然产物,是姜黄素的主要代谢产物,可抑制 CYP2C9和 CYP3A4,具有很强的抗氧化和心脏保护作用。 |