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BAY-899 Sale

目录号 : GC61746

BAY-899是一种口服有效和选择性的促黄体生成激素受体(LH-R)拮抗剂,对hLH(人LH)和rLH(大鼠LH)的IC50分别为185nM和46nM。BAY-899可以降低性激素水平。

BAY-899 Chemical Structure

Cas No.:2471967-92-5

规格 价格 库存 购买数量
5 mg
¥990.00
现货
10 mg
¥1,800.00
现货
25 mg
¥3,600.00
现货
50 mg
¥5,760.00
现货
100 mg
¥9,450.00
现货

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产品文档

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产品描述

BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels[1].

BAY-899 (oral; 12.5 mg/kg/day; for 8 days) shows an efficiency to reduce serum estradiol levels in intact female rats[1]. BAY-899 (iv of 0.5 mg/kg or po of 2 mg/kg) has a t1/2 of 11 hours and 12 hours for iv and po. And the Cmax is 0.97 kg/L and 0.24 kg/L for iv and po[1]. Animal Model: Intact female rats[1]

[1]. Wortmann L, et al. Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels In Vivo. J Med Chem. 2019 Oct 31.

Chemical Properties

Cas No. 2471967-92-5 SDF
Canonical SMILES O=C(N1[C@@H](C2=CC=C(F)C=C2)C3=C(N=CC=C3)CC1)NC4=CN=C(OC5=CC=C(F)C=C5)N=C4
分子式 C25H19F2N5O2 分子量 459.45
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1 mg 5 mg 10 mg
1 mM 2.1765 mL 10.8826 mL 21.7652 mL
5 mM 0.4353 mL 2.1765 mL 4.353 mL
10 mM 0.2177 mL 1.0883 mL 2.1765 mL
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Research Update

Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo

J Med Chem 2019 Nov 27;62(22):10321-10341.PMID:31670515DOI:10.1021/acs.jmedchem.9b01382

The human luteinizing hormone receptor (hLH-R) is a member of the glycoprotein hormone family of G-protein-coupled receptors (GPCRs), activated by luteinizing hormone (hLH) and essentially involved in the regulation of sex hormone production. Thus, hLH-R represents a valid target for the treatment of sex hormone-dependent cancers and diseases (polycystic ovary syndrome, uterine fibroids, endometriosis) as well as contraception. Screening of the Bayer compound library led to the discovery of tetrahydrothienopyridine derivatives as novel, small-molecule (SMOL) hLH-R inhibitors and to the development of BAY-298, the first nanomolar hLH-R antagonist reducing sex hormone levels in vivo. Further optimization of physicochemical, pharmacokinetic, and safety parameters led to the identification of BAY-899 with an improved in vitro profile and proven efficacy in vivo. BAY-298 and BAY-899 serve as valuable tool compounds to study hLH-R signaling in vitro and to interfere with the production of sex hormones in vivo.