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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- CAS No.: 1615208-41-7
- Formule: C42H48N6O8
- Masse moléculaire:764.87
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
pKi: 10.4 (M3 muscarinic receptor), 11.4 (β2-adrenergic receptors)[1]
IC50: ~50 μM (calcium channel)[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.
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Animal Model:Guinea pigs[1]
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Dosage:0.3 and 1 nM/kg
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Administration:Intratracheal administration; single dosage
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Result:Inhibited bronchoconstriction in a dose-dependent manner.
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Animal Model:Guinea pigs[1]
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Dosage:500 nM/kg (Pharmacokinetic Analysis)
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Administration:Intratracheal administration; single dosage
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Result:Sustained exposure up to 72 h and the appropriate gradual decline which is suggestive of no accumulation risk.
Showed very low systemic exposure.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1615208-41-7
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Masse moléculaire 764.87
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Formule C42H48N6O8
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHF-6366 Related Classifications
HY-151198 Related Classifications
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