Vimirogant (VTP-43742) | RORγt inhibitor | Probechem Biochemicals

Chemical Structure : VTP-43742

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VTP-43742 (Vimirogant, VTP43742)

货号: PC-60452Not For Human Use, Lab Use Only.

VTP-43742 (Vimirogant, VTP43742) is a highly potent, selective, oral RORγt inverse agonist with Ki/IC50 of 3.5/17 nM respectively.

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生物&药学活性

VTP-43742 (Vimirogant, VTP43742) 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	552.657
分子式	C27H35F3N4O3S
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

参考文献

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

VTP-43742 (Vimirogant, VTP43742)

生物&药学活性

物理化学性质&存储条件

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VTP-43742 (Vimirogant, VTP43742)

生物&药学活性

物理化学性质&存储条件

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