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Cytochrome P450

Cytochrome P450相关产品(72)
货号 产品名 中文名称 产品描述
SJ-MX0675 Memantine hydrochloride 盐酸美金刚

Memantine hydrochloride (D-145 hydrochloride) 是一种温和的 NMDA 受体 (NMDA receptor) 非竞争性拮抗剂,(体外IC50 = 0.5 ~ 1.5 μM),与离子通道位点结合。 Memantine hydrochloride 还能够抑制 CYP2B6 和 CYP2D6,Ki值分别为0.51 μM和84.4 μM。

SJ-MX0897 Verapamil hydrochloride 盐酸维拉帕米

Verapamil hydrochloride (CP-16533-1 hydrochloride) 是一种L-型钙通道 (calcium channel) 阻滞剂,可抑制正常心脏组织以及房室和窦房结中钙的缓慢向内流动。Verapamil hydrochloride是一种有效的口服活性的第一代 P 糖蛋白 (permeability-glycoprotein,P-gp) 抑制剂。Verapamil hydrochloride 能也抑制 CYP3A4,并可用于高血压,心律不齐和心绞痛的研究。

SJ-MX0968A Abiraterone Acetate 乙酸阿比特龙酯 Abiraterone Acetate是一种口服、有效、选择性和不可逆的甾体类CYP17A1 抑制剂。Abiraterone Acetate是Abiraterone前药,具有抗雄激素活性。Abiraterone acetateis 是一种口服的雄性激素 androgen 生物合成抑制剂。
SJ-MX0968B Abiraterone 阿比特龙

Abiraterone是一种口服、有效、选择性和不可逆的甾体类CYP17A1 抑制剂,具有抗雄激素活性。Abiraterone抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶(17α-hydroxylase)和 17,20-裂合酶(17,20-lyase )活性,IC50 值 分别为 2.5 nM 和 15 nM。

SJ-MX3603 Orteronel (TAK-700) Orteronel (TAK-700) is a potent, orally available, and highly selective inhibitor of 17,20-lyase (CYP17A1; IC50 value 19 nM and 48 nM for human and rat respectively) and of correlated androgen synthesis. TAK 700 exhibits no affinity for CYP11B 1and CYP3A4 (IC50 values >1000 nM and >10000 nM resp.), nor for other isoforms of the human CYP enzyme (IC50 values >14000 nM). When given orally to monkeys at a dose of 1 mg/kg, TAK 700 markedly reduced serum testosterone and DHEA at 5 h after administration.TAK 700 was selected for evaluation in patients in phase III clinical trials for the potential treatment of prostate cancer.
SJ-MX1200 DMU2139 DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
SJ-MX2993 APD668 APD668 is a potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat. APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM).
SJ-MX2513 Atovaquone 阿托伐醌 Atovaquone (Atavaquone) is a broad-spectrum antiprotozoal agent that is active against Plasmodium, Toxoplasma, and Babesia, among other protozoa. It inhibits complex III activity on dihydroorotate in isolated P. falciparum and P. yoelii mitochondria more potently than in rat liver mitochondria (EC50s = 0.95, 0.94, and 510 nM, respectively) and depolarizes the mitochondrial membrane in P. yoelii-infected mouse erythrocytes (EC50 = 260 nM). Atovaquone also inhibits transport mediated by human breast cancer resistance protein (BCRP) and P-glycoprotein in membrane vesicles (IC50s = 0.23 and 6.8 μM, respectively.
SJ-MX2566 Clomethiazole 氯美噻唑 Clomethiazole is a positive allosteric modulator at the barbiturate/picrotoxin site of the GABAA receptor. It acts as a sedative and hypnotic agent.
SJ-MX1622 1-Aminobenzotriazole 1-氨基苯并三唑 1-Aminobenzotriazole 是细胞色素 P450 (P450) 的非特异且不可逆抑制剂。
SJ-MX1599 Brassinazole 芸苔素唑;(Rac)-芸苔素唑; (Rac)-油菜素唑 (Rac)-Brassinazole 是三唑型化合物,是油菜素甾醇 (BR) 生物合成抑制剂。(Rac)-Brassinazole 增加 CYP90B 在 BR 生物合成中的抑制作用。
SJ-MX2526 Bergaptol Bergaptol is a novel and potent skin-photosensitizing hydroxyfurocoumarin.
SJ-MX2564 Clobetasol propionate 丙酸氯倍他索 Clobetasol propionate (formerly CGP-9555, CCl-4725; CGP9555; CCl4725; Clobex Cosvate; Temovate; Olux Tenovate) is a topical corticosteroid used as an anti-inflammatory for treatment of various skin disorders including eczema and psoriasis.
SJ-MX2590 Doxepin hydrochloride 盐酸多塞平 Doxepin hydrochloride is a highly potent Histamine H1 Receptor (histamine H1) antagonist. Doxepin hydrochloride also binds to histamine H4 receptor. Doxepin hydrochloride is an inhibitor of AR and mAChR. Doxepin hydrochloride is a dibenzoxepin analogue and tricyclic antidepressant with antipruritic and sedative activities. Doxepin also has antagonistic effects on histamine (H1 and H2), 5-HT2, alpha-1 adrenergic, and muscarinic receptors. The antipruritic effect of this agent is the result mediated through inhibition of histamine receptors.
SJ-MX2593 1-Ethynylnaphthalene 1-乙炔萘;1-乙炔基萘 1-Ethynylnaphthalene 是细胞色素 P450 1B1 的选择性抑制剂。
SJ-MX2653 Metyrapone 美替拉酮 Metyrapone is a drug used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism). It blocks cortisol synthesis by reversibly inhibiting steroid 11β-hydroxylase. This stimulates ACTH secretion, which in turn increases plasma 11-deoxycortisol levels.
SJ-MX2697 Proadifen hydrochloride Proadifen hydrochloride is an inhibitor of drug metabolism and CYTOCHROME P-450 ENZYME SYSTEM activity.
SJ-MX2728 Ticlopidine Ticlopidine (PCR 5332) 是一种抗血栓前药,作为非竞争性的变构 CD39 抑制剂,IC50 为 81.7 µM。Ticlopidine 阻断 NTPDase 同工酶,对 NTPDase2 和 NTPDase3 的 IC50 分别为 170 µM 和 149 µM。Ticlopidine 是 CYP2C19 人肝细胞色素的抑制剂。Ticlopidine 抑制 CYP2C9 和 CYP3A4,IC50 值分别为 26.0 和 32.3 µM。
SJ-MX3286 Gemfibrozil 吉非罗齐

吉非罗齐(Pilder;CI-719;CI719;Lopid;Jezil; Lipur;Trialmin)是一种有效的抗高甘油三酯/降脂药物,作为过氧化物增殖激活受体-α(PPARα)的激活剂/拮抗剂。它已被批准用于治疗高胆固醇血症和高甘油三酯血症。

SJ-MX1105 TMS TMS ((E)-2,3',4,5'-tetramethoxystilbene) 是一种选择性和竞争性 CYP1B1 抑制剂,IC50 为 6 nM,Ki 值为 3 nM。TMS 对 CYP1A1 (IC50=300 nM) 和 CYP1A2 (IC50=3.1 μM) 的抑制作用较小。TMS 是白藜芦醇的甲基化衍生物,具有抗癌活性。