2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. mAChR Adrenergic Receptor Calcium Channel
  4. CHF-6366

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).

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CHF-6366 Chemical Structure

CHF-6366 Chemical Structure

CAS No. : 1615208-41-7

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CHF-6366 Related Antibodies

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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α adrenergic receptor β adrenergic receptor

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Description

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].

IC50 & Target

pKi: 10.4 (M3 muscarinic receptor), 11.4 (β2-adrenergic receptors)[1]
IC50: ~50 μM (calcium channel)[1]
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].

Lung Plasma
Cmax 28400 ng/g 126 ng/mL
Tmax 0.083 h 0.083 h
AUClast 460361 ng/g·h 460 ng/mL·h
AUCinf 725199 ng/g·h 661 ng/mL·h
half-life 49.2 h 15.4 h

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

Animal Model: Guinea pigs[1]
Dosage: 0.3 and 1 nM/kg
Administration: Intratracheal administration; single dosage
Result: Inhibited bronchoconstriction in a dose-dependent manner.
Animal Model: Guinea pigs[1]
Dosage: 500 nM/kg (Pharmacokinetic Analysis)
Administration: Intratracheal administration; single dosage
Result: Sustained exposure up to 72 h and the appropriate gradual decline which is suggestive of no accumulation risk.
Showed very low systemic exposure.
Clinical Trial
Molecular Weight

764.87

Formula

C42H48N6O8
CAS No.
SMILES

O=C(C1=NN(C)C(COC2=CC=CC([C@H](C3=CC=CC=C3)NC(O[C@H]4CN5CCC4CC5)=O)=C2)=C1)OCCCCNC[C@H](O)C6=CC=C(O)C7=C6C=CC(N7)=O
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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CHF-6366 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.

Keywords:

CHF-63661615208-41-7CHF6366CHF 6366mAChRAdrenergic ReceptorCalcium ChannelMuscarinic acetylcholine receptorBeta ReceptorCa2+ channelsCa channelsbronchoconstrictionchronic obstructive pulmonary diseaseCOPDguinea pigintratrachealInhibitorinhibitorinhibit

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