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).
For research use only. We do not sell to patients.
- CAS No.: 1615208-41-7
- Formula: C42H48N6O8
- Molecular Weight:764.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
pKi: 10.4 (M3 muscarinic receptor), 11.4 (β2-adrenergic receptors)[1]
IC50: ~50 μM (calcium channel)[1]
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1615208-41-7
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Molecular Weight 764.87
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHF-6366 Related Classifications
HY-151198 Related Classifications
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