产品
编 号：F746148
分子式：C42H48N6O8
分子量：764.87
分子式：C42H48N6O8
分子量：764.87
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CAS No: 1615208-41-7
产品详情
生物活性：
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).
体内研究：
CHF-6366 (0.3 and 1 nM/kg; intratracheal administration; single dosage) inhibits bronchoconstriction in a dose-dependent manner.CHF-6366 (500 nM/kg; intratracheal administration; single dosage) exhibits low systemic exposure and no accumulation risk.Pharmacokinetic Parameters of CHF-6366 in lung and plasma of guinea pig (intratracheal administration, 500 nM/kg).Lung Plasma
Cmax28400 ng/g126 ng/mL
Tmax0.083 h0.083 h
AUClast460361 ng/g·h460 ng/mL·h
AUCinf725199 ng/g·h661 ng/mL·h
half-life49.2 h15.4 h
Animal Model:Guinea pigs
Dosage:0.3 and 1 nM/kg
Administration:Intratracheal administration; single dosage
Result:Inhibited bronchoconstriction in a dose-dependent manner.
Animal Model:Guinea pigs
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.
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).
体内研究：
CHF-6366 (0.3 and 1 nM/kg; intratracheal administration; single dosage) inhibits bronchoconstriction in a dose-dependent manner.CHF-6366 (500 nM/kg; intratracheal administration; single dosage) exhibits low systemic exposure and no accumulation risk.Pharmacokinetic Parameters of CHF-6366 in lung and plasma of guinea pig (intratracheal administration, 500 nM/kg).Lung Plasma
Cmax28400 ng/g126 ng/mL
Tmax0.083 h0.083 h
AUClast460361 ng/g·h460 ng/mL·h
AUCinf725199 ng/g·h661 ng/mL·h
half-life49.2 h15.4 h
Animal Model:Guinea pigs
Dosage:0.3 and 1 nM/kg
Administration:Intratracheal administration; single dosage
Result:Inhibited bronchoconstriction in a dose-dependent manner.
Animal Model:Guinea pigs
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.
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