PeptideDB

CHF-6366

CAS: 1615208-41-7 F: C42H48N6O8 W: 764.87

CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, res
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Bioactivity CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD)[1].
Target pKi: 10.4 (M3 muscarinic receptor), 11.4 (β2-adrenergic receptors)IC50: ~50 μM (calcium channel)
In Vivo CHF-6366 (0.3 and 1 nM/kg; intratracheal administration; single dosage) inhibits bronchoconstriction in a dose-dependent manner[1].CHF-6366 (500 nM/kg; intratracheal administration; single dosage) exhibits low systemic exposure and no accumulation risk[1].Pharmacokinetic Parameters of CHF-6366 in lung and plasma of guinea pig (intratracheal administration, 500 nM/kg)[1].
Name CHF-6366
CAS 1615208-41-7
Formula C42H48N6O8
Molar Mass 764.87
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Carzaniga L, et al. Discovery of Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β2 Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases. J Med Chem. 2022 Aug 11;65(15):10233-10250.