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40

抑制剂 & 化合物

8

天然产物

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Cat. No. Product Name Target Signaling Pathways
T76147 3α-Hydroxysteroid dehydrogenase

3α-Hydroxysteroid dehydrogenase(3α-HSD) 是一种由 AKR1C4 基因编码的酶,可以催化 3-酮类甾体转化为 3α-羟基化合物。3α-Hydroxysteroid dehydrogenase 在雄激素 DHT 的失活中起重要作用,可以将 DHT 转化成雄激素活性很弱的 3α-雄烷二醇,可用于多毛症研究。
T0238 2-(Acetyloxy)-3-Methylbenzoic Acid

Others Others
2-(Acetyloxy)-3-Methylbenzoic Acid 用于 qHTS 测定羟基类固醇 (17-β) 脱氢酶 4、HSD17B4 的抑制剂,活性值为 19.95 μM。
T68664 Epostane

Win-32729

Dehydrogenase Metabolism
Epostane (Win-32729) 是一种 3β- 羟基类固醇脱氢酶抑制剂,通过抑制 3β-羟类固醇脱氢酶发挥作用,阻断黄体酮的产生。
T67903 11β-HSD1 inibitor 17

Dehydrogenase Metabolism
11β-HSD1 inibitor 17 是11β-羟基类固醇脱氢酶(11β-HSD1)抑制剂。
T9594 BI-187004

Dehydrogenase Metabolism
BI-187004 是一种 11β-羟基类固醇脱氢酶 1 抑制剂。
T14151 AKR1C1-IN-1

NADPH Metabolism
AKR1C1-IN-1 是高选择性 AKR1C1抑制剂(Ki:4 nM)。
T14388 AZD 4017

Dehydrogenase Metabolism
AZD 4017 是高效的、选择性的11β-HSD1抑制剂,IC50为 7 nM。
T71394 BMS-823778

BMS-823778 is an orally available potent and selective inhibitor of 11-β-hydroxysteroid-dehydrogenase 1 (11βHSD-1). BMS-823778 is a potential therapeutic agent for type 2 diabetes mellitus (T2DM).
T3542 BVT-14225

BVT 14225

Dehydrogenase Metabolism
BVT-14225 是一种选择性的11β羟基类固醇脱氢酶1型(11β-HSD1)抑制剂(IC50:52 nM)。
T13100 TC HSD 21

Dehydrogenase Metabolism
TC HSD 21 是一种有效且高度选择性的 17β-羟基类固醇脱氢酶 3 型抑制剂 (IC50 = 14 nM)。
T77576 17β-HSD10-IN-1

Dehydrogenase; Endogenous Metabolite Metabolism
17β-HSD10-IN-1 是一种可口服且具有血脑通透性和有效性的 17β-羟基类固醇脱氢酶 10 型 (17β-HSD10) 抑制剂,可用于研究阿尔茨海默症。
T1473 Trilostane

曲洛斯坦,Win 24540,曲洛司坦

Dehydrogenase Metabolism
Trilostane (Win 24540) 是一种3 β-羟化类固醇脱氢酶抑制剂,能够作用于库兴氏综合征。
T73446 BI‑3231

Dehydrogenase Metabolism
BI‑3231 是一种具有选择性和高效性的羟基类固醇 17ß-脱氢酶 13 HSD17B13 抑制剂,抑制 hHSD17B13 和 mHSD17B13。BI‑3231 可用于研究酒精相关肝损伤、纤维化和肝硬化。
T77606 WAY-311610

Dehydrogenase Metabolism
WAY-311610是一种11β-羟基类固醇脱氢酶HSD11B1抑制剂,抑制11β-HSD1酶,IC = 0.34μM。可用于研究神经性疼痛、炎症性疼痛和枕神经痛。
T22458 WEHL-04

7-Bromo-1,2,3,4-tetrahydroquinoline,7-溴-1,2,3,4-四氢喹啉

Others Others
WEHL-04 是一种中间体,用于制备(异喹啉基磺酰基)苯甲酸,作为 5 型 71-β-羟基类固醇脱氢酶 AKR1C3 的抑制剂。它还用于合成 2-氨基八氢环戊二烯-3a-羧酰胺作为有效的 CCR2 拮抗剂。
T16510 PF-915275

Dehydrogenase Metabolism
PF-915275 是口服有效的人 11β-羟基类固醇脱氢酶1型选择性抑制剂,Ki 为 2.3 nM,在 HEK293 细胞中的EC50为 15 nM 。它对人和猴原代肝细胞中可的松向皮质醇的转化具有剂量依赖性,EC50分别为 20 nM 和 100 nM。
T63569 HSD-016

HSD-016 是选择性的、有效的、口服具有活力的 1 型 11β-羟类固醇脱氢酶(11β-HSD1)抑制剂,能够作用于人 11β-HSD1 (IC50: 11 nM)、小鼠 11β-HSD1 (IC50: 1 nM)、大鼠 11β-HSD1 (IC50: 8 nM)。HSD-016 能够用于研究 2 型糖尿病。
T60149 11β-HSD1-IN-11

Dehydrogenase Metabolism
11β-HSD1-IN-11 是一种有效的、具有竞争性的 11- β-羟基类固醇脱氢酶1 (11β-HSD1)抑制剂,对大鼠和人的 11β-HSD1具有抑制作用,IC50 分别为 0.34 μM 和 0.13 μM。11β-HSD1- in -11是一种作为的化合物。11β-HSD1-IN-11是一种参与调节各种生理过程的激素,例如代谢、炎症和应激反应。11β-HSD1-IN-11是治疗代谢紊乱、肥胖和某些炎症状况的潜在化合物。
T26528 ABT-384

ABT-384 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1.
T28727 SCH-451659

SCH-451659 is an 17β-hydroxysteroid dehydrogenases (17β-HSDs) inhibitor.
T33423 MK-0916

MK 0916

MK-0916 is a 11β-hydroxysteroid dehydrogenase type 1 inhibitor indicated for the treatment of type 2 diabetes and metabolic syndrome as well as obesity-related diseases.
T81010 Tetrahydro-11-dehydrocorticosterone

Tetrahydro-11-dehydrocorticosterone 是一种抑制11β-HSD(11β-羟类固醇脱氢酶)的化合物。
T28796 SKI2852

SK I2852,SKI-2852

SKI2852 is a highly Potent, selective, and orally bioavailable inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). hHSD1 IC50 = 2.9nM; mHSD1 IC50 = 1.6nM.
T10946 D4-abiraterone

Abiraterone D4A metabolite,CB-7627,Δ4-Abiraterone

Androgen Receptor Endocrinology/Hormones
D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.
T61716 Steroid sulfatase/17β-HSD1-IN-1

Steroid sulfatase/17β-HSD1-IN-1 is a highly effective inhibitor of both steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) activities, displaying an IC50 value of 28 nM against cellular human steroid sulfatase. This compound holds significant potential for investigating estrogen-dependent diseases [1].
T79886 HSD17B13-IN-3

HSD17B13-IN-3(化合物2)是一种有效的HSD17B13抑制剂,但不具备细胞实验活性。
T79885 HSD17B13-IN-2

HSD17B13-IN-2(化合物1)是一种高效的HSD17B13抑制剂,显示出显著的细胞实验活性。
T72249 BMS-823778 hydrochloride

BMS-823778 hydrochloride为一种高效、选择性的口服11β-HSD1抑制剂,其对人11β-HSD1的IC50值为2.3 nM。
T61593 11β-HSD1-IN-6

11β-HSD1-IN-6 is a potent inhibitor of 11β hydroxysteroid dehydrogenase enzymes (11β-HSDs). These enzymes are responsible for catalyzing the conversion of the active glucocorticoids, corticosterone or cortisol, to their respective inactive forms, 11-dehydrocorticosterone (11-DHC) and cortisone. The compound 11β-HSD1-IN-6 specifically targets and inhibits 11β-HSD-1, effectively modulating the interconversion of these glucocorticoids. [1]
T80817 WAY-328127

WAY-328127是一种活性分子,适用于生化反应研究。
T60203 INCB13739

INCB13739是一种具有口服活性、高效、选择性及组织特异性的11β-HSD1抑制剂,对11β-HSD1酶的IC50为3.2 nM,对11β-HSD1 PBMC的IC50为1.1 nM。适用于2型糖尿病(T2DM)和肥胖的研究。
T35572 Adenosine 3',5'-diphosphate sodium salt

3'-Phosphoadenosine 5'-phosphate

Endogenous Metabolite Metabolism
Adenosine 3',5'-diphosphate sodium salt 是一种羟类固醇磺基转移酶 (hydroxysteroid sulfotransferases) 抑制剂,是一种腺嘌呤核苷酸,在戊糖核糖的 3'和 5'位置含有一个磷酸基团。Adenosine 3',5'-diphosphate (sodium salt)是 3'-phosphoadenosine 5'-phosphosulfonate (PAPS) 的产物,是磺基转移酶(SULTs)的辅助因子,已被用于研究 SULTs 的动力学特性和结构。
T12663 (Rac)-BMS-816336

Dehydrogenase Metabolism
(Rac)-BMS-816336 (Compound 6n) 是 BMS-816336 的外消旋体。(Rac)-BMS-816336 是人和小鼠 11β-羟类固醇脱氢酶 1 型 (11β-HSD1) 的有效抑制剂,其 IC50分别为 10 nM 和 68 nM,并具有良好的代谢稳定性 。
T68808 11-Dehydrocorticosterone

11-Dehydrocorticosterone is an endogenous mineralocorticoid. It increases Na+/K+-ATPase mRNA expression in vascular smooth muscle cells and inhibits aldosterone action in B. marinus toad bladder tissue in a concentration-dependent manner. 11-Dehydrocorticosterone decreases the sodium/creatine ratio and increases the potassium/creatine ratio in rat urine in a dose-dependent manner in a model of 11β-hydroxysteroid dehydrogenase inhibition induced by carbenoxolone. Chronic administration 11-dehydro...
T70763 KR-67607

KR-67607, also known as NTX-101 is novel selective 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. KR-67607 decreased 4-hydroxynonenal expression and increased antioxidant and mucus secretion in BAC-treated rat eyes. KR-67607 showed its protective effects against ischemia-reperfusion-induced eye injury. KR-67607 effectively reduced cortisol levels in mouse eyes and maintained the trabecular meshwork (TM) structure in the presence of transient ischemic stress. Furthermore, KR-67607 rever...
T79459 17β-HSD10-IN-2

Endogenous Metabolite Metabolism
17β-HSD10-IN-2(compound 11)是一款基于苯并噻唑脲结构的17β-羟基类固醇脱氢酶10型(17β-HSD10)抑制剂,后者为一种具有多功能性的线粒体酶。该抑制剂未触发线粒体脱靶现象,且不具备细胞毒性或神经毒性。17β-HSD10-IN-2可用于研究阿尔茨海默病(AD)和激素依赖型癌症。
T62236 Steroid sulfatase/17β-HSD1-IN-3

Steroid sulfatase/17β-HSD1-IN-3 (compound 19) 是一种双重的类固醇硫酸酯酶 (STS) 和 17β-羟基类固醇脱氢酶 1 型 (17β HSD1) 抑制剂。Steroid sulfatase/17β-HSD1-IN-3 对 hSTS 的活性具有不可逆的抑制作用 (IC50: 27 nM)。Steroid sulfatase/17β-HSD1-IN-3 能够用于研究子宫内膜异位症及其他雌激素依赖性疾病。
T61979 Steroid sulfatase/17β-HSD1-IN-4

Steroid sulfatase/17β-HSD1-IN-4 (compound 37) 是一种类固醇硫酸酯酶 (STS) 和 17β-羟基类固醇脱氢酶 1 型 (17β HSD1) 双重抑制剂。Steroid sulfatase/17β-HSD1-IN-4 对 hSTS 的活性抑制作用不可逆,IC50为 63 nM。Steroid sulfatase/17β-HSD1-IN-4 在子宫内膜异位症及其他雌激素依赖性疾病方面有研究价值。
T81092 Steroid sulfatase/17β-HSD1-IN-5

Steroid sulfatase/17β-HSD1-IN-5 是一种不可逆抑制剂,针对类固醇硫酸酯酶(STS),同时也是17β-羟甾类固醇脱氢酶1型(17β-HSD1)的可逆且选择性抑制剂,表现出对17β-HSD1的IC50为43 nM,对17β-HDS1为6.2 μM。该化合物主要用于研究代谢性疾病,特别是子宫内膜异位症。
T74729 18β-Glycyrrhetyl-3-O-sulfate

18β-Glycyrrhetyl-3-O-sulfate(Glycyrrhetic acid 3-O-(hydrogen sulfate))是一种对2型11β-羟基类固醇脱氢酶(11β-HSD2)具有高效抑制作用的化合物,其在大鼠肾微粒体中的IC50值为0.10 µM。作为Glycyrrhetinic acid (GA)的重要代谢产物,18β-Glycyrrhetyl-3-O-sulfate同时也是有机阴离子转运蛋白(OAT)1和OAT3的底物。此外,该化合物展示出抗炎活性,并可能用于假性醛固酮增多症的研究领域。

化合物

3α-Hydroxysteroid dehydrogenase
Cat.No: T76147
Synonym:
Target:
2-(Acetyloxy)-3-Methylbenzoic Acid
Cat.No: T0238
Synonym:
Target: Others
Epostane
Cat.No: T68664
Synonym: Win-32729
Target: Dehydrogenase
11β-HSD1 inibitor 17
Cat.No: T67903
Synonym:
Target: Dehydrogenase
BI-187004
Cat.No: T9594
Synonym:
Target: Dehydrogenase
AKR1C1-IN-1
Cat.No: T14151
Synonym:
Target: NADPH
AZD 4017
Cat.No: T14388
Synonym:
Target: Dehydrogenase
BMS-823778
Cat.No: T71394
Synonym:
Target:
BVT-14225
Cat.No: T3542
Synonym: BVT 14225
Target: Dehydrogenase
TC HSD 21
Cat.No: T13100
Synonym:
Target: Dehydrogenase
17β-HSD10-IN-1
Cat.No: T77576
Synonym:
Target: Dehydrogenase, Endogenous Metabolite
Trilostane
Cat.No: T1473
Synonym: 曲洛斯坦,Win 24540,曲洛司坦
Target: Dehydrogenase
BI‑3231
Cat.No: T73446
Synonym:
Target: Dehydrogenase
WAY-311610
Cat.No: T77606
Synonym:
Target: Dehydrogenase
WEHL-04
Cat.No: T22458
Synonym: 7-Bromo-1,2,3,4-tetrahydroquinoline,7-溴-1,2,3,4-四氢喹啉
Target: Others
PF-915275
Cat.No: T16510
Synonym:
Target: Dehydrogenase
HSD-016
Cat.No: T63569
Synonym:
Target:
11β-HSD1-IN-11
Cat.No: T60149
Synonym:
Target: Dehydrogenase
ABT-384
Cat.No: T26528
Synonym:
Target:
SCH-451659
Cat.No: T28727
Synonym:
Target:
MK-0916
Cat.No: T33423
Synonym: MK 0916
Target:
Tetrahydro-11-dehydrocorticosterone
Cat.No: T81010
Synonym:
Target:
SKI2852
Cat.No: T28796
Synonym: SK I2852,SKI-2852
Target:
D4-abiraterone
Cat.No: T10946
Synonym: Abiraterone D4A metabolite,CB-7627,Δ4-Abiraterone
Target: Androgen Receptor
Steroid sulfatase/17β-HSD1-IN-1
Cat.No: T61716
Synonym:
Target:
HSD17B13-IN-3
Cat.No: T79886
Synonym:
Target:
HSD17B13-IN-2
Cat.No: T79885
Synonym:
Target:
BMS-823778 hydrochloride
Cat.No: T72249
Synonym:
Target:
11β-HSD1-IN-6
Cat.No: T61593
Synonym:
Target:
WAY-328127
Cat.No: T80817
Synonym:
Target:
INCB13739
Cat.No: T60203
Synonym:
Target:
Adenosine 3',5'-diphosphate sodium salt
Cat.No: T35572
Synonym: 3'-Phosphoadenosine 5'-phosphate
Target: Endogenous Metabolite
(Rac)-BMS-816336
Cat.No: T12663
Synonym:
Target: Dehydrogenase
11-Dehydrocorticosterone
Cat.No: T68808
Synonym:
Target:
KR-67607
Cat.No: T70763
Synonym:
Target:
17β-HSD10-IN-2
Cat.No: T79459
Synonym:
Target: Endogenous Metabolite
Steroid sulfatase/17β-HSD1-IN-3
Cat.No: T62236
Synonym:
Target:
Steroid sulfatase/17β-HSD1-IN-4
Cat.No: T61979
Synonym:
Target:
Steroid sulfatase/17β-HSD1-IN-5
Cat.No: T81092
Synonym:
Target:
18β-Glycyrrhetyl-3-O-sulfate
Cat.No: T74729
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2207 Adrenosterone

肾上腺甾酮,11-ketoandrostenedione,11-oxoandrostenedione,Reichstein's substance G

Androgen Receptor; Endogenous Metabolite Endocrinology/Hormones; Metabolism
Adrenosterone (11-ketoandrostenedione) 是一种人内源性代谢物,由肾上腺皮质产生。Adrenosterone 是一种竞争性羟基类固醇脱氢酶 1 抑制剂。它是一种的类固醇激素,具有较弱的雄激素特性。它是一种膳食补充剂,能够减少脂肪并提高肌肉质量。它能够抑制人类癌细胞的转移进展。
T14001 11-Beta-hydroxyandrostenedione

4-雄烯-11β-醇-3,17-二酮,NSC-17102,4-Androsten-11β-ol-3,17-dione

Endogenous Metabolite Metabolism
11-Beta-hydroxyandrostenedione (NSC-17102) 是主要存在于肾上腺的类固醇,也是 11β-羟基类固醇脱氢酶同工酶抑制剂。随着 4-androstenedione 的提高,通过测量血浆中的11-Beta-hydroxyandrostenedione,能够区分高雄激素血症的肾上腺或卵巢起源。
T0522 Diammonium Glycyrrhizinate

甘草酸二铵,Glycyrrhizin

Dehydrogenase Metabolism
Diammonium Glycyrrhizinate (Glycyrrhizin) 是分离自甘草中的化合物,有抗炎作用。
TJS0341 7-Amino-4-(trifluoromethyl)coumarin

香豆素151,Coumarin 151,AFC,7-氨基-4-(三氟甲基)香豆素

5-HT Receptor GPCR/G Protein; Neuroscience
7-Amino-4-(trifluoromethyl)coumarin (Coumarin 151) 是一种荧光标记物,其激发和发射波长分别为400和500 nm,可用来灵敏的检测蛋白酶。
T17057 Tetrahydrocortisol

Others Others
The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase activity. Tetrahydrocortisol is cortisol metabolite.
TN5230 Vibralactone D

Others Others
Vibralactones D shows weak inhibitory activities against isozymes of 11beta-hydroxysteroid dehydrogenases (HSD) with IC(50) values of 85.7 microM (human HSD1), 295.2 microM (mouse HSD1), and 87.1 microM (human HSD2).
TCA2511 11Beta-hydroxyprogesterone

Sodium Channel Membrane transporter/Ion channel
The progesterone derivatives 11 alpha- and 11 beta-hydroxyprogesterone are potent inhibitors of 11 beta-hydroxysteroid dehydrogenase (isoforms 1 and 2) in vitro and can confer mineralocorticoid activity on corticosterone in the rat in vivo. 11beta-Hydroxyprogesterone acts as a mineralocorticoid agonist in stimulating Na+ absorption in mammalian principal cortical collecting duct cells.
T83364 3-Acetyl-11-keto-ursolic acid

3-Acetyl-11-keto-ursolic acid (Compound 18)为Eriobotrya japonica叶中提取的三萜类化合物,其抑制11b-羟基类固醇脱氢酶1 (11b-HSD1) 的特性使其在抗糖尿病研究中具有应用潜力。

天然产物

Adrenosterone
Cat.No: T2207
Synonym: 肾上腺甾酮,11-ketoandrostenedione,11-oxoandrostenedione,Reichstein's substance G
Target: Androgen Receptor, Endogenous Metabolite
11-Beta-hydroxyandrostenedione
Cat.No: T14001
Synonym: 4-雄烯-11β-醇-3,17-二酮,NSC-17102,4-Androsten-11β-ol-3,17-dione
Target: Endogenous Metabolite
Diammonium Glycyrrhizinate
Cat.No: T0522
Synonym: 甘草酸二铵,Glycyrrhizin
Target: Dehydrogenase
7-Amino-4-(trifluoromethyl)coumarin
Cat.No: TJS0341
Synonym: 香豆素151,Coumarin 151,AFC,7-氨基-4-(三氟甲基)香豆素
Target: 5-HT Receptor
Tetrahydrocortisol
Cat.No: T17057
Synonym:
Target: Others
Vibralactone D
Cat.No: TN5230
Synonym:
Target: Others
11Beta-hydroxyprogesterone
Cat.No: TCA2511
Synonym:
Target: Sodium Channel
3-Acetyl-11-keto-ursolic acid
Cat.No: T83364
Synonym:
Target:
TargetMol Loading
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