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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-BI 730357
BI 730357

Chemical Structure : BI 730357

CAS No.: 1817773-66-2

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BI 730357 (Bevurogant, BI-730357)

货号: PC-20041Not For Human Use, Lab Use Only.

BI 730357 (Bevurogant, BI-730357) is a potent selective RORγt antagonist with IC50 of 150 nM in reporter gene assays (RGA), inhibits the secretion of IL-17A of PBMCs with IC50 of 24 nM.

规格 价格 库存 数量
5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BI 730357 (Bevurogant, BI-730357) is a potent selective RORγt antagonist with IC50 of 150 nM in reporter gene assays (RGA), inhibits the secretion of IL-17A of PBMCs with IC50 of 24 nM.
BI 730357 showed potent IL-17 inhibition in the human whole blood setting (IC50=140 nM), inhibited human RORγ-mediated IL-22 production (IC50=43 nM) in human PBMCs.
BI 730357 shows no off-target activity in the typical screening panels of receptors and kinases.
BI 730357 (0.3, 3, and 30 mg/kg, oral) demonstrated significant inhibition of IL-17A mRNA in in vivo murine IL-23 minicircle model, and inhibition of the disease-relevant biomarkers S100a8, S100a9, and β-defensin in the skin (ED50 < 0.3 mg/kg).

物理化学性质&存储条件

分子量 532.62
分子式 C26H28N8O3S
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)-2-(4-cyclopropyl-6-methylpyrimidin-5-yl)-8-(1-cyclopropylethyl)-6-(((5-(methylsulfonyl)pyridin-2-yl)methyl)amino)pteridin-7(8H)-one

参考文献

1. Harcken C, et al. ACS Med Chem Lett. 2021 Jan 5;12(1):143-154.

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