PeptideDB

CHF5407

CAS: 1004312-94-0 F: C27H25BrF4N2O3S W: 613.46

CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affini
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Bioactivity CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity[1].
Target human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors
Invitro CHF5407 has a very slow dissociation from M3 receptors (hM3; t1/2=166 min) and markedly short-acting at M2 receptors (hM2; t1/2=31 min)[1]. CHF5407 produces a potent (pIC50=9.0-9.6) and long-lasting (up to 24 h) inhibition of M3 receptor-mediated contractile responses to carbachol in the guinea pig isolated trachea and human isolated bronchus[1].
In Vivo CHF5407 (0.1, 0.3, 1 nmol/kg; intratracheally; 100 ul; sigle dose) exerted a dose-dependent and potent inhibition of ACh-induced (20 g/kg; i.v.) bronchospasm, with an ED50 value of 0.15 nmol/kg in guinea pigs (450-550 g)[1].
Name CHF5407
CAS 1004312-94-0
Formula C27H25BrF4N2O3S
Molar Mass 613.46
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]. G Villetti, et al. Bronchodilator activity of (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino] carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407), a potent, long-acting, and selective muscarinic M3 rec