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BI 730357

Chemical Structure : BI 730357

CAS No.: 1817773-66-2

BI 730357 (Bevurogant, BI-730357)

Catalog No.: 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.

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50 mg $358 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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).

Physicochemical Properties

M.Wt 532.62
Formula C26H28N8O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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