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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1615208-41-7
- 分子式: C42H48N6O8
- 分子量:764.87
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
pKi: 10.4 (M3 muscarinic receptor), 11.4 (β2-adrenergic receptors)[1]
IC50: ~50 μM (calcium channel)[1]
体内実験
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1615208-41-7
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分子量 764.87
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CHF-6366 関連分類
HY-151198 関連分類
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