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29

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T14301 Apararenone

MT-3995

Glucocorticoid Receptor Endocrinology/Hormones
Apararenone (MT-3995) 是一种新型的、非甾体类盐皮质激素受体 (mineralocorticoid receptor) 拮抗剂,正在开发用于糖尿病性肾病和非酒精性脂肪性肝炎的研究。
T9022 AZD9977

AZD 9977

Glucocorticoid Receptor Endocrinology/Hormones
AZD9977 是一种选择性的,有效的,具有口服活性的盐皮质激素受体 (MR) 调节剂,可用于研究心力衰竭和慢性肾病。
T4277 Osilodrostat

LCI699

Glucocorticoid Receptor; Others; Hydroxylase Endocrinology/Hormones; Metabolism; Others
Osilodrostat (LCI699) 是一种有效的人11β-羟化酶和醛固酮合成酶抑制剂,IC50分别值为2.5 和0.7nM。
T15246 Esaxerenone

艾沙利酮,XL-550,CS-3150

Glucocorticoid Receptor Endocrinology/Hormones
Esaxerenone (XL-550) 是高效的、选择性的非类固醇盐皮质激素受体拮抗剂。
T0476 Spironolactone

安体舒通,螺内酯,SC9420,Abbolactone

Glucocorticoid Receptor; Androgen Receptor; Autophagy Autophagy; Endocrinology/Hormones
Spironolactone (SC9420) 是一种可口服的醛固酮盐皮质激素受体拮抗剂,IC50值为 24 nM。它也是雄激素受体拮抗剂,促进足细胞自噬,IC50值为 77 nM。
T0083 Eplerenone

Epoxymexrenone,CGP 30083,依普利酮,SC-66110

Glucocorticoid Receptor Endocrinology/Hormones
Eplerenone (CGP 30083) 是一种竞争性的、选择性的、具有口服活性的醛固酮 (aldosterone) 拮抗剂,IC50=138 nM。它对孕酮,雄激素,雌激素和糖皮质激素受体的亲和力低,可用于研究高血压和心肌梗死后的心力衰竭。
T17217 Vamorolone

地塞米松EP杂质E,VBP15

Glucocorticoid Receptor; NF-κB Endocrinology/Hormones; NF-κB
Vamorolone (VBP15) 是一种首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。它抑制 (NF-κB) 抑制作用,并降低了激素的影响。它改善肌营养不良,无副作用。
T3096 Canrenoate potassium

坎利酸钾,Potassium aldadiene,Canrenoic acid potassium salt,Potassium canrenoate,Soldactone

Glucocorticoid Receptor Endocrinology/Hormones
Canrenoate potassium (Soldactone) 是一种有效的竞争性盐皮质激素受体 (mineralocorticoid receptor) 拮抗剂,是一种释放 canrenone 的前药。它作为一种利尿剂,用于高血压的研究。
T1666L Fludrocortisone

9α-fluorocortisol,9α-Fludrocortisone,Florinef,9α-fluorohydrocortisone,氟氢可的松,Fludrocortisone acetate,Astonin,9α-Fluorcortisol

Others Others
Fludrocortisone (Florinef) 是一种合成皮质类固醇,具有中等的糖皮质激素效力和更大的盐皮质激素效力。Fludrocortisone (Florinef) 可用于治疗低血压的研究。
T1666 Fludrocortisone acetate

9α-Fluorcortisol acetate,9α-Fludrocortisone acetate,醋酸氟氢可的松,9α-fluorocortisol acetate

Glucocorticoid Receptor; Autophagy Autophagy; Endocrinology/Hormones
Fludrocortisone acetate (9α-Fludrocortisone acetate) 是一种合成的盐皮质激素,可减少尿液中钠丢失量,也用于增加血压,有用于阿狄森氏病的研究潜力。
T21395 Finerenone

BAY948862,BAY-948862,BAY94-8862,非奈利酮,BAY 94-8862,BAY-94-8862,BAY 948862

Glucocorticoid Receptor Endocrinology/Hormones
Finerenone (BAY-948862) 是一种选择性、具有口服活性的、非甾体类盐皮质激素受体拮抗剂 (IC50=18 nM)。与糖皮质激素受体、雄激素受体和孕酮受体相比,它表现出良好的选择性 (>500-fold)。它在心肾疾病研究中具有潜在的应用前景,如 2 型糖尿病和慢性肾脏疾病。
T1541 Drospirenone

ZK 3059,屈螺酮,Dihydrospirorenone

Glucocorticoid Receptor; Estrogen/progestogen Receptor; Progesterone Receptor; Androgen Receptor; COX Endocrinology/Hormones; Immunology/Inflammation; Neuroscience; Others
Drospirenone (ZK 3059) 是spironolactone 的类似物,是一种合成的孕酮。
T32368 KB-74935

KB 74935

Others Others
KB-74935是一种酶抑制剂,是一种矿物皮质激素受体拮抗剂,可用于治疗 胆固醇、低血脂、神经系统疾病和阿尔茨海默病。
T13881 Dicirenone

SC26304

ATPase; Glucocorticoid Receptor Endocrinology/Hormones; Membrane transporter/Ion channel
Dicirenone (SC26304) 对盐皮质激素受体 (MR)有抑制作用,对醛固酮对尿 K+:Na+ 比例的调节和 醛固酮与肾细胞质和核受体结合有抑制作用。
T0094 Budesonide

Entocort,Pulmicort,布地奈德,Rhinocort

Glucocorticoid Receptor Endocrinology/Hormones
Budesonide (Pulmicort) 是吸入型糖皮质类固醇,是一种口服具有活性的糖皮质激素受体激动剂。它能够减小肺部肿瘤的体积,逆转 DNA 低度甲基化,调节基因的 mRNA 表达。它是能够用于哮喘的抗炎药。
T17291 ZK 216348

(+)-ZK 216348

Others Others
ZK 216348 also binds to Progesterone and mineralocorticoid receptors (IC50s: 20.4 nM and 79.9 nM, respectively). ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist (IC50: 20.3 nM). ZK 216348 has an anti-inflammatory activity similar to
T23272 RU 28318, potassium salt

Others Others
mineralocorticoid receptor (MR) antagonist
T16502 PF-3882845

Others Others
PF-3882845 also binds to the progesterone receptor (the binding IC50: 310 nM). PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy.
T68699 Oxprenoate Free Base

Oxprenoate Free Base is a mineralocorticoid receptor (MR) antagonist, inhibiting aldosterone production and secretion.
T26157 RU 752

RU-752,RU752

RU 752 is an antagonist of mineralocorticoid receptor that inhibits aldosterone synthesis.
T36129 21-hydroxy Eplerenone

21-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone . It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4.
TC0008 Desoxycorticosterone pivalate

DOCP

Others Others
Deoxycorticosterone (DOCP) is a mineralocorticoid and is an analog of deoxycorticosterone. Deoxycorticosterone pivalate is used in the treatment of canine low adrenal cortex hormones.
T37064 6β-hydroxy Eplerenone

6β-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone .1 It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4. |1. Cook, C.S., Berry, L.M., Kim, D.H., et al. Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: Differential metabolism by CYP3A4 and CYP3A5. Drug Metab. Dispos. 30(12), 1344-1351 (2002).
T69323 Dexamethasone sodium succinate

Dexamethasone sodium succinate is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regul...
T38448 (Rac)-Finerenone

(Rac)-Finerenone,(Rac)-BAY 94-8862

Rac-Finerenone, also known as (Rac)-BAY 94-8862, is the racemate derivative of Finerenone, a selective third-generation nonsteroidal mineralocorticoid receptor antagonist (MR) that is taken orally. With an IC50 value of 18 nM, Finerenone exhibits exceptional selectivity against the glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).
T36381 Aldosterone 21-sulfate (sodium salt)

Aldosterone 21-sulfate is a metabolite of the steroid hormone aldosterone .1It reduces the sodium-to-potassium ratio in rat urine when administered at doses ranging from 10 to 100 μg, indicating mineralocorticoid activity that is less than 1% that of aldosterone.2 1.Grose, J.H., Nowaczynski, W., Kuchel, O., et al.Isolation of aldosterone urinary metabolites, glucuronides and sulfateJ. Steroid Biochem.4(6)551-566(1973) 2.Jowett, T.P., and Slater, J.D.H.Aldosterone 21-sulphate in manJ. Steroid. Bi...
T68765 Spirorenone

Spirorenone is an androstadienone derivative as a highly effective aldosterone antagonist. Spirorenone is 8.6 times as potent as spironolactone, but showed a lower affinity for the mineralocorticoid receptors. In phase I clinical trials Spirorenone was absorbed with a half-life of 20-30 min, achieving maximum concentrations of about 100 ng/ml (10 mg) and 260 ng/ml (40 mg) after 1-2 h. Disposition of the parent drug was biphasic with half-lives of 50-60 min (distribution) and 5-6 h (elimination)....
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...
T68009 prorenoate

Prorenoate 是一种甾体醛固酮拮抗剂,具有保钾利尿作用。Prorenoate 可拮抗醛固酮在肾元中盐皮质激素受体的活性,从而阻止钠的重吸收。这会干扰钠/钾交换器,导致钠和水排泄,同时减少钾排泄。

化合物

Apararenone
Cat.No: T14301
Synonym: MT-3995
Target: Glucocorticoid Receptor
AZD9977
Cat.No: T9022
Synonym: AZD 9977
Target: Glucocorticoid Receptor
Osilodrostat
Cat.No: T4277
Synonym: LCI699
Target: Glucocorticoid Receptor, Others, Hydroxylase
Esaxerenone
Cat.No: T15246
Synonym: 艾沙利酮,XL-550,CS-3150
Target: Glucocorticoid Receptor
Spironolactone
Cat.No: T0476
Synonym: 安体舒通,螺内酯,SC9420,Abbolactone
Target: Glucocorticoid Receptor, Androgen Receptor, Autophagy
Eplerenone
Cat.No: T0083
Synonym: Epoxymexrenone,CGP 30083,依普利酮,SC-66110
Target: Glucocorticoid Receptor
Vamorolone
Cat.No: T17217
Synonym: 地塞米松EP杂质E,VBP15
Target: Glucocorticoid Receptor, NF-κB
Canrenoate potassium
Cat.No: T3096
Synonym: 坎利酸钾,Potassium aldadiene,Canrenoic acid potassium salt,Potassium canrenoate,Soldactone
Target: Glucocorticoid Receptor
Fludrocortisone
Cat.No: T1666L
Synonym: 9α-fluorocortisol,9α-Fludrocortisone,Florinef,9α-fluorohydrocortisone,氟氢可的松,Fludrocortisone acetate,Astonin,9α-Fluorcortisol
Target: Others
Fludrocortisone acetate
Cat.No: T1666
Synonym: 9α-Fluorcortisol acetate,9α-Fludrocortisone acetate,醋酸氟氢可的松,9α-fluorocortisol acetate
Target: Glucocorticoid Receptor, Autophagy
Finerenone
Cat.No: T21395
Synonym: BAY948862,BAY-948862,BAY94-8862,非奈利酮,BAY 94-8862,BAY-94-8862,BAY 948862
Target: Glucocorticoid Receptor
Drospirenone
Cat.No: T1541
Synonym: ZK 3059,屈螺酮,Dihydrospirorenone
Target: Glucocorticoid Receptor, Estrogen/progestogen Receptor, Progesterone Receptor, Androgen Receptor, COX
KB-74935
Cat.No: T32368
Synonym: KB 74935
Target: Others
Dicirenone
Cat.No: T13881
Synonym: SC26304
Target: ATPase, Glucocorticoid Receptor
Budesonide
Cat.No: T0094
Synonym: Entocort,Pulmicort,布地奈德,Rhinocort
Target: Glucocorticoid Receptor
ZK 216348
Cat.No: T17291
Synonym: (+)-ZK 216348
Target: Others
RU 28318, potassium salt
Cat.No: T23272
Synonym:
Target: Others
PF-3882845
Cat.No: T16502
Synonym:
Target: Others
Oxprenoate Free Base
Cat.No: T68699
Synonym:
Target:
RU 752
Cat.No: T26157
Synonym: RU-752,RU752
Target:
21-hydroxy Eplerenone
Cat.No: T36129
Synonym:
Target:
Desoxycorticosterone pivalate
Cat.No: TC0008
Synonym: DOCP
Target: Others
6β-hydroxy Eplerenone
Cat.No: T37064
Synonym:
Target:
Dexamethasone sodium succinate
Cat.No: T69323
Synonym:
Target:
(Rac)-Finerenone
Cat.No: T38448
Synonym: (Rac)-Finerenone,(Rac)-BAY 94-8862
Target:
Aldosterone 21-sulfate (sodium salt)
Cat.No: T36381
Synonym:
Target:
Spirorenone
Cat.No: T68765
Synonym:
Target:
11-Dehydrocorticosterone
Cat.No: T68808
Synonym:
Target:
prorenoate
Cat.No: T68009
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3033 Deoxycorticosterone acetate

醋酸去氧皮质酮,DOC acetate,Cortexone acetate,11-Deoxycorticosterone acetate,醋酸脱氧皮质酮

Glucocorticoid Receptor; Endogenous Metabolite; Adrenergic Receptor Endocrinology/Hormones; GPCR/G Protein; Metabolism; Neuroscience
Deoxycorticosterone acetate (Cortexone acetate) 是肾上腺产生的类固醇激素,具有盐皮质激素活性,并作为醛固酮的前体。
T0354 Canrenone

6,7-Dehydro-7α-desthioacetylspironolactone,SC9376,Aldadiene,坎利酮,RP-11614,SC14266

Glucocorticoid Receptor; Endogenous Metabolite Endocrinology/Hormones; Metabolism
Canrenone (SC14266) 是一种醛固酮 (aldosterone) 拮抗剂,广泛用作利尿剂。
TN3910 Ecdysone

Apoptosis; ATPase; Glucocorticoid Receptor; Potassium Channel; Sodium Channel; Endogenous Metabolite; Autophagy Apoptosis; Autophagy; Endocrinology/Hormones; Membrane transporter/Ion channel; Metabolism
Ecdysone 是存在于昆虫和草药中的主要类固醇激素,可以激活盐皮质激素受体并诱导细胞凋亡。Ecdysone 的活性代谢物 20-羟基蜕皮激素在协调发育过渡和体内稳态睡眠调节中起重要作用。
T20302 Deoxycorticosterone

Desoxycorticosterone,去氧皮质酮,Desoxycorticosteronum,Desoxycortone

Endogenous Metabolite Metabolism
Deoxycorticosterone (Desoxycortone) 是由肾上腺产生的类固醇代谢物。 Deoxycorticosterone 是醛固酮前体,具有盐皮质激素活性。
T39991 18-Oxocortisol

18-Oxocortisol is a cortisol derivative generated by aldosterone synthase (CYP11B2). It acts as a naturally occurring mineralocorticoid agonist and serves as a biomarker in adrenal vein sampling.
T19186 Aldosterone

Others Others
Aldosterone is the primary mineralocorticoid. Aldosterone is synthesized and secreted in response to renin-angiotensin system activation or high dietary potassium by the zona glomerulosa of the adrenal cortex.
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.

天然产物

Deoxycorticosterone acetate
Cat.No: T3033
Synonym: 醋酸去氧皮质酮,DOC acetate,Cortexone acetate,11-Deoxycorticosterone acetate,醋酸脱氧皮质酮
Target: Glucocorticoid Receptor, Endogenous Metabolite, Adrenergic Receptor
Canrenone
Cat.No: T0354
Synonym: 6,7-Dehydro-7α-desthioacetylspironolactone,SC9376,Aldadiene,坎利酮,RP-11614,SC14266
Target: Glucocorticoid Receptor, Endogenous Metabolite
Ecdysone
Cat.No: TN3910
Synonym:
Target: Apoptosis, ATPase, Glucocorticoid Receptor, Potassium Channel, Sodium Channel, Endogenous Metabolite, Autophagy
Deoxycorticosterone
Cat.No: T20302
Synonym: Desoxycorticosterone,去氧皮质酮,Desoxycorticosteronum,Desoxycortone
Target: Endogenous Metabolite
18-Oxocortisol
Cat.No: T39991
Synonym:
Target:
Aldosterone
Cat.No: T19186
Synonym:
Target: Others
11Beta-hydroxyprogesterone
Cat.No: TCA2511
Synonym:
Target: Sodium Channel
TargetMol Loading
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