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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-Vimirogant hydrochloride
Vimirogant hydrochloride

Chemical Structure : Vimirogant hydrochloride

CAS No.: 1802678-42-7

Vimirogant hydrochloride (VTP-43742 hydrochloride)

货号: PC-26233Not For Human Use, Lab Use Only.

Vimirogant hydrochloride (VTP-43742) is a highly potent, selective, oral RORγt inverse agonist with Ki/IC50 of 3.5/17 nM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Vimirogant hydrochloride (VTP-43742) is a highly potent, selective, oral RORγt inverse agonist with Ki/IC50 of 3.5/17 nM respectively.
VTP-43742 exhibits >1,000-fold selectivity versus the RORα and RORβ.
VTP-43742 inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation.
VTP-43742 inhibits the secretion of IL-17A from activated hPBMCs (IC50=18 nM) and human whole blood (IC50=192 nM).
VTP-43742 shows potential for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis.

物理化学性质&存储条件

分子量
分子式 C27H35F3N4O3S.xHCl
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-((5-(ethylsulfonyl)pyridin-2-yl)methyl)-7-isopropyl-6-(((1r,4S)-4-(trifluoromethyl)cyclohexyl)methyl)-6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-3-carboxamide hydrochloride

参考文献

1. Pandya VB, et al. J Med Chem. 2018 Jul 16. doi: 10.1021/acs.jmedchem.8b00588.

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