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.

Product information

CAS Number: 1004312-94-0

Molecular Weight: 613.46

Formula: C27H25BrF4N2O3S

Chemical Name: (3R)-3-{[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]carbamoyl]oxy}-1-[2-oxo-2-(thiophen-2-yl)ethyl]-1-azabicyclo[2.2.2]octan-1-ium bromide

Smiles: [Br-].O=C(C[N+]12C[C@H](OC(=O)N(CC3=CC(F)=C(F)C(F)=C3)C3C=CC=C(F)C=3)C(CC1)CC2)C1=CC=CS1

InChiKey: BDUVQZSIMOIWQB-JTOZIPDCSA-M

InChi: InChI=1S/C27H25F4N2O3S.BrH/c28-19-3-1-4-20(13-19)32(14-17-11-21(29)26(31)22(30)12-17)27(35)36-24-16-33(8-6-18(24)7-9-33)15-23(34)25-5-2-10-37-25;/h1-5,10-13,18,24H,6-9,14-16H2;1H/q+1;/p-1/t18?,24-,33?;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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). 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.

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).

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