P450

Cytochrome P450 are a family of heme-containing monoxygenases catalyzing the metabolism of xenobiotics in the body where P450 enzymes use O2 and two electrons provided by NAD(P)H with the help of redox partner flavoproteins and iron-sulfur proteins to catalyze the monooxygenation of a variety of substrates. Based on how electrons from NAD(P)H are delivered to the catalytic site, P450 enzymes are divided into four classes, including Class I requiring both an FAD-containing reductase and an iron sulfur redoxin, Class II requiring only an FAD/FMN-containg P450 reductase, Class III requiring no electron donor and Class IV requiring electrons directly from NAD(P)H.

Products for P450

Cat.No. 产品名称 Information
GC32991 Cecropin B
天蚕丝抗菌肽
Cecropin B是一种多肽抗菌素，对大肠杆菌及其他多种革兰氏阴性菌具有强效抗菌活性，具有广谱的抗菌活性。
GC32855 Furafylline
呋拉茶碱
Furafylline，作为治疗哮喘的长效茶碱替代品，是甲基黄嘌呤衍生物。
GC32419 BI 689648 BI689648是一种新型的，高选择性醛固酮合酶抑制剂，能抑制CYP11B1和CYP11B2，其IC50值分别为310和2.1nM。
GC32257 Carbosulfan
丁硫克百威
Carbosulfan强效抑制CYP3A4,适度抑制CYP1A1/2和CYP2C19。
GC32160 Tebuconazole
戊唑醇
A triazole fungicide
GC31791 Veledimex (INXN-1001)
INXN-1001; RG-115932
Veledimex (INXN-1001) (INXN-1001) 是昆虫蜕皮激素蜕皮激素的合成类似物，是专有基因治疗启动子系统的口服活性激活剂配体。
GC31479 BMS-819881 BMS-819881是一种黑色素浓缩激素受体1(MCHR1)拮抗剂，结合大鼠MCHR1，Ki值为7nM。BMS-819881还有效且选择性地作用于CYP3A4，EC50为13μM.
GC31464 CDD3505 CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
GC31460 CDD3506 CDD3506可以通过诱导肝CYP3A的活动，来提高高密度脂蛋白胆固醇(HDL)的水平。
GC31422 MCH-1 antagonist 1
MCH-1antagonist1是一种有效的黑色素浓缩激素1(MCH-1)拮抗剂，Ki值为2.6nM。MCH-1antagonist1还抑制CYP3A4，IC50为10μM。
GC31141 Antihistamine-1 Antihistamine-1是能够渗透血脑屏障的H1-抗组胺药(Ki=6.9nM),它也是CYP2D6和hERG通道的抑制剂，其IC50值分别为5.4和0.8μM。
GC30985 Methysticin (DL-Methysticin)
麻醉椒苦素,DL-Methysticin; (±)-Methystici
A natural kavalactone
GC30966 Olivetol
橄榄醇
An Analytical Reference Standard
GC30705 Veledimex S enantiomer (INXN-1001 S enantiome)
INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
Veledimex S 对映体 (INXN-1001 S enantiomer) 是 veledimex 的 S 对映体。 Veledimex 是专有基因治疗启动子系统的口服激活剂配体，也是 CYP3A4/5 的中度抑制剂和底物。
GC30681 Revexepride Revexepride是一种高度选择性的5-HT4receptor激动剂，也是潜在的CYP3A4enzyme诱导剂，可用于治疗胃食管返流疾病。
GC30479 Dihydromethysticin ((+)-Dihydromethysticin)
二氢麻醉椒素,(+)-Dihydromethysticin
A kavalactone with diverse biological activities
GC30459 Senecionine (Senecionan-11,16-dione, 12-hydroxy-)
千里光宁,Senecionan-11,16-dione, 12-hydroxy-; Aureine; Senecionin
A pyrrolizidine alkaloid with hepatotoxic properties
GC30424 (-)-Cephaeline dihydrochloride (NSC 32944)
盐酸吐根酚碱,(-)-Cephaeline dihydrochloride; NSC 32944
(-)-Cephaeline dihydrochloride (NSC 32944) 是一种选择性 CYP2D6 抑制剂，IC50 为 121 μM.
GC19483 MS-PPOH A potent, selective inhibitor of microsomal CYP450 epoxidase activity
GC19416 DMU2139 DMU2139是一种有效的CYP1B1抑制剂，IC₅₀值为9nM。
GC19415 DMU2105 DMU2105 是一种有效且特异性的 CYP1B1 抑制剂，对 CYP1B1 和 CYP1A1 的 IC50 分别为 10 nM 和 742 nM。
GC19301 Pradefovir mesylate
Remofovir mesylate
Pradefovir mesylate 是肝脏 CYP3A4 的良好底物。
GC18879 CAY10662 A urea derivative of 17(18)-EpETE
GC18817 3β-hydroxy-5-Cholestenoic Acid
3β-hydroxy-5-CA, Cholesterol-26-carboxylic Acid
An active cholesterol metabolite
GC18791 Prostaglandin H1
前列腺素H1
The precursor to all 1-series prostaglandins and thromboxanes
GC18783 13,14-dihydro-15-keto Prostaglandin E1
13,14-二氢-15-酮-前列腺素E1
An inactive metabolite of PGE₁
GC18706 SR 9186
ML368
A selective inhibitor of CYP3A4
GC18698 CAY10665 A stable bioisostere of the antiarrhythmic 17,18-EET
GC18654 8-hydroxy Loxapine
8-OH Loxapine
A loxapine metabolite
GC18622 (2'S)-Nicotine-1-oxide
(2'S)-尼古丁氧化物
A nicotine metabolite
GC18582 5'-hydroxy Meloxicam
5'-羟基美洛昔康
A metabolite of meloxicam
GC18539 4-Hydroxyretinoic acid (4-HRA)
维甲酸杂质
4-Hydroxyretinoic acid (4-HRA)是一种天然存在的，由全反式视黄酸（ATRA）经细胞色素P450酶代谢生成的主要代谢产物。
GC18527 4'-hydroxy Flurbiprofen
4-羟基氟吡洛芬
A major active metabolite of flurbiprofen
GC18460 Roquefortine C
异烟棒曲霉素 C
A mycotoxin
GC18425 4-hydroxy Atorvastatin lactone
P-羟基阿伐他汀内酯
A metabolite of atorvastatin
GC18335 6β-hydroxy Dexamethasone
6-羟基地塞米松
A metabolite of dexamethasone
GC18286 (R)-Mephenytoin
美芬妥英,(-)-Mephenytoin
An enantiomer of mephenytoin
GC18219 6-hydroxy Warfarin
3-(Α-丙酮基苄基)-4,6-二羟基香豆素
A phase I metabolite of (+)-warfarin
GC10136 Tienilic Acid
替宁酸,Ticrynafen; ANP 3624
Suicide substrate of CYP 2C9
GC15244 Thienyldecyl Isothiocyanate An antiproliferative isothiocyanate
GC11540 HET0016
N-hydroxy-N'-(4-n-butyl-2-methylphenyl)Formamidine
HET0016 是一种高选择性的20-羟基花生四烯酸（20-HETE）合成酶抑制剂，对重组CYP4A1、CYP4A2和CYP4A3催化20-HETE合成作用的IC₅₀值分别为17.7nM, 12.1nM和20.6nM。
GC17112 Uniconazole
烯效唑,S 3307D,XE 1019D
A plant growth regulator
GC12262 2-Phenyl-2-(1-piperidinyl)propane
1-(1-甲基-1-苯基乙基)哌啶
A selective inhibitor of CYP2B6
GC15056 β-Nicotyrine
二烯烟碱,α-Nicotyrine,NSC 127943,NSC 407276
β-Nicotyrine是一种尼古丁的热解产物，可与细胞色素P450 (CYP) isoforms CYP2A6和CYP2A13结合，并能更有效地抑制CYP2A6的活性
GC13836 2,3-dihydrothieno-Thiadiazole Carboxylate
MTCC
Selective CYP450 inhibitor
GC11758 4-phenyl-5-methyl-1,2,3-Thiadiazole
5-甲基-4-苯基-1,2,3-噻二唑,NSC 358739

CYP2B4 and CYP2E1 inhibitor
GC13470 Rhapontigenin
丹叶大黄素
Rhapontigenin（丹叶大黄素）是一种有效的细胞色素P4501A1选择性灭活剂，IC₅₀为0.4μM，对P4501A1的选择性分别是P4501A2和P4501B1的400倍和23倍。
GC12892 Doxepin (hydrochloride)
盐酸多塞平
A tricyclic antidepressant
GC11638 Sulfaphenazole
磺胺苯吡唑
Sulfaphenazole是一种磺胺类抗菌药物。它竞争性地抑制细菌二氢叶酸合酶，阻断细菌叶酸合成，从而抑制细菌生长和繁殖。
GC16423 Monoacetylphloroglucinol
2,4,6-三羟基苯乙酮; 2,4,6-trihydroxyacetophenone; 1-(2,4,6-Trihydroxyphenyl)ethanone
单乙酰间苯三酚（2,4,6-三羟基苯乙酮）是从姜黄中提取的苯乙酮糖苷的苷元部分，具有降低胆固醇的活性。