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Chemical Structure : BI 1015550
CAS No.: 1423719-30-5
Catalog No.: PC-49676Not For Human Use, Lab Use Only.
BI 1015550 (Nerandomilast, VRN024219) is a potent, selective PDE4B inhibitor that preferentially inhibits hydrolysis of cAMP by PDE4B with IC50 of 10 nM, weakly inhibits PDE4A/4C/4D (IC50=248/8700/91 nM, respectively).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $128 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
| 100 mg | Get quote |
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BI 1015550 (Nerandomilast, VRN024219) is a potent, selective PDE4B inhibitor that preferentially inhibits hydrolysis of cAMP by PDE4B with IC50 of 10 nM, weakly inhibits PDE4A/4C/4D (IC50=248/8700/91 nM, respectively).
BI 1015550 displays no significant activity agianst human PDE7A and human PDE3A, and PDE1C, PDE9A, human PDE2A and PDE5 at 10 uM.
BI 1015550 inhibited LPS-induced TNF- α release with an IC50 35 nM in human PBMCs, inhibited phytohemagglutinin P-induced IL-2 release with IC50 of 9 nM.
BI 1015550 completely inhibited LPS-stimulated TNF-α release with an IC50 in rat whole blood, inhibited TNF-α release up to 70–80% with an IC50 of 670 nM human whole blood.
BI 1015550 (0.01, 0.1, and 1 mg/kg, p.o.) inhibited LPS-stimulated TNF-α release in whole blood ex vivo in mice with ED50 of 0.04 mg/kg.
BI 1015550 (0.01, 0.1, and 1 mg/kg, p.o.) inhibited LPS-induced lung neutrophil influx in male Wistar rats with an ED50 of 0.1 mg/kg.
BI 1015550 inhibited α-SMA protein expression of TGF-β-stimulated IPF-LF with an IC50 of 210 nM, showed a synergistic effect in combination with Nintedanib on fibroblast proliferation.
BI 1015550 is a promising oral clinical candidate for the treatment of idiopathic pulmonary fibrosis (IPF) and other fibro-proliferative diseases.
| M.Wt | 448.97 | |
| Formula | C20H25ClN6O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
[1-({(5R)-2-[4-(5-chloropyrimidin-2-yl)piperidin-1-yl]-5-oxido-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl}amino)cyclobutyl]methanol |
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