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Chemical Structure : BI 730357
CAS No.: 1817773-66-2
Catalog No.: PC-20041Not For Human Use, Lab Use Only.
BI 730357 (Bevurogant, BI-730357) is a potent selective RORγ antagonist with IC50 of 150 nM in reporter gene assays (RGA), inhibits the secretion of IL-17A of PBMCs with IC50 of 24 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $498 | In stock | |
| 10 mg | $758 | In stock | |
| 25 mg | $1280 | In stock | |
| 100 mg | Get quote | ||
| 1 g | Get quote |
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BI 730357 (Bevurogant, BI-730357) is a potent selective RORγ 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).
| M.Wt | 532.62 | |
| Formula | C26H28N8O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Harcken C, et al. ACS Med Chem Lett. 2021 Jan 5;12(1):143-154.
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