1. GPCR/G Protein Neuronal Signaling
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  3. CHF5407

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.

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CHF5407 Chemical Structure

CHF5407 Chemical Structure

CAS No. : 1004312-94-0

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Description

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].

IC50 & Target

human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors[1]

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)[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

613.46

Formula

C27H25BrF4N2O3S

CAS No.
SMILES

O=C(C1=CC=CS1)C[N+]23C[C@@H](C(CC3)CC2)OC(N(C4=CC(F)=CC=C4)CC5=CC(F)=C(F)C(F)=C5)=O.[Br-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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CHF5407 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CHF5407
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HY-U00302
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