P450
Cytochrome P450 (P450) is a superfamily of heme-thiolate enzymes that are ubiquitous in almost all biological systems. There are more than 35,000 P450 enzymes that have been isolated from all biological organisms, with exception of some primitive prokaryotes, such as Escherichia coli, which are believed to have emerged before the evolution of P450. Members of the same P450 family share ≥40% sequence homology, whereas members of the same P450 subfamily share ≥55% sequence homology. In humans, there are 18 P450 families comprised of 60 P450 enzymes, of which the majority is microsomal P450 belong to CYP2, CYP3 and CYP4 families. P450-mediated metabolism plays a critical role determining the onset and duration of drug action. Hepatic microsomal P450 enzymes, typically CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C18, CYP2C19, CYP2D6, CYP2E1 and CYP3A4, determine how much will be the half-life in the body for most of drugs.
References
1.El-Sherbeni AA, El-Kadi AO. Drug Metab Rev. 2017;49(1):1–17.
References
1.El-Sherbeni AA, El-Kadi AO. Drug Metab Rev. 2017;49(1):1–17.
Metabolic Enzyme/Protease
11β-HSD(15)
15-PGDH(1)
ACC(10)
ACE(15)
AChE(47)
Adenylate Cyclase(12)
ALDH(14)
Aldose Reductase(5)
Aminopeptidase(19)
BACE(19)
Casein Kinase(51)
CAT(5)
Cathepsin(9)
CETP(13)
COMT(2)
CPG2(1)
CYPs(6)
Decarboxylase(3)
Dehydrogenase(131)
DGAT(4)
Dopamine beta-hydroxylase(2)
DPP(32)
Elastase(6)
FAAH(28)
Factor Xa(31)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
IMPDH(2)
LDH(2)
LDL(8)
Lipase(17)
Lipid(12)
MAGL(6)
MAO(72)
MMP(78)
NAMPT(12)
Neprilysin(7)
Other Targets(10)
P450(112)
PAI-1(9)
Phosphatase(95)
Phospholipase(65)
PPAR(115)
Protein Phosphatase/PTP(6)
Renin(8)
Retinoid Receptor(37)
SCD(6)
Steroid Sulfatase (STS)(2)
Thioredoxin(1)
TPH(5)
Transferase(37)
Vitamin(44)
Xanthine Oxidase (XAO)(11)
P450
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CYP1B1-IN-7
产品货号 : M37571
cas no: 52601-58-8
CYP1B1-IN-7 is a selective and potent CYP1B1 inhibitor showing cytotoxic effects in docetaxel-resistant CYP1B1 overexpressing MCF-7 cell lines, and can be used in synergistic treatment of cancer with anticancer compounds. -
Opevesostat
产品货号 : M37000
cas no: 2231294-96-3
Opevesostat 是一种胆固醇侧链裂解酶 (CYP11A1) 抑制剂。 -
Albaconazole
产品货号 : M36847
cas no: 187949-02-6
Albaconazole (W-0027) is a small molecule fungal cytochrome P450 family member 51 (fungal CYP51A1) inhibitor. It is used in the treatment of fungal infections, skin and musculoskeletal disorders, and can be used in the study of vulvovaginal candidiasis, Chagas disease and genitourinary disorders. -
CYP1B1-IN-5
产品货号 : M36491
cas no: 176442-56-1
CYP1B1-IN-5 (Compound 6q) 是一种有效的、选择性的细胞色素 P450 1B1 (CYP1B1) 抑制剂,IC50 为 4.7 nM。 -
CYP1B1-IN-4
产品货号 : M36490
cas no: 2685779-55-7
CYP1B1-IN-4 是一种选择性 CYP1B1 抑制剂 (IC50=0.2 nM),是一种 2,4-二芳基噻唑化合物。CYP1B1-IN-4 的细胞毒性低,在人和大鼠肝微粒体中均具有稳定性。