11β-HSD
11β-HSD catalyze interconversion of active cortisol and corticosterone with inert cortisone and 11-dehydrocorticosterone. 11β-HSD type 1, a predominant reductase in most intact cells, catalyzes the regeneration of active glucocorticoids, thus amplifying cellular action; 11β-HSD2 is a high-affinity dehydrogenase that inactivates glucocorticoids. In the distal nephron, 11β-HSD2 ensures that only aldosterone is an agonist at mineralocorticoid receptors (MR).The 11β-HSDs thus illuminate the emerging biology of intracrine control, afford important insights into human pathogenesis, and offer new tissue-restricted therapeutic avenues.
References:
1.Chapman K, et al. Physiol Rev. 2013 Jul;93(3):1139-206.
References:
1.Chapman K, et al. Physiol Rev. 2013 Jul;93(3):1139-206.
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)
11β-HSD
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HSD-016
产品货号 : M16784
cas no: 946396-92-5
HSD-016 (HSD016) 是一种强效、选择性且有效的 11β-HSD1 抑制剂,对小鼠和人 11β-HSD1 的 IC50 分别为 149 和 530 nM。 -
INCB13739
产品货号 : M16343
cas no: 872506-67-7
INCB13739 (INCB-13739) 是一种有效、选择性、口服 11βHSD1 抑制剂 (IC50=1.1 nM),与其他脱氢酶、糖皮质激素和盐皮质激素受体相比具有高选择性。 -
PF-915275
产品货号 : M16219
cas no: 857290-04-1
一种特异性有效的人类 11β-HSD1 抑制剂,Ki 为 2.3 nM,体外 HEK293 EC50 为 15 nM。 -
BVT-2733
产品货号 : M14299
cas no: 376640-41-4
小鼠 11β-HSD1 的非甾体异构体选择性抑制剂,Ki 为 1 uM。 -
BVT-14225
产品货号 : M14298
cas no: 376638-65-2
一种选择性 11β-羟基类固醇脱氢酶 1 型 (11β-HSD1) 抑制剂,IC50 为 52 nM。