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BI 1015550

Chemical Structure : BI 1015550

CAS No.: 1423719-30-5

BI 1015550 (Nerandomilast, VRN024219)

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).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 448.97
Formula C20H25ClN6O2S
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

[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

References

1. Herrmann FE, et al. Front Pharmacol. 2022 Apr 20;13:838449.

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