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

CHF-6366 是一种有效的 M3 毒蕈碱 (muscarinic) 拮抗剂和 β2 肾上腺素能受体 (adrenergic receptors) 激动剂，pKi 分别为 10.4 和 11.4。CHF-6366 也是一种弱钙离子通道 (calcium channel) 抑制剂 (IC50~50 μM)。CHF-6366 抑制豚鼠的支气管收缩。CHF-6366 可用于慢性阻塞性肺疾病 (COPD) 的研究。

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CHF-6366 Chemical Structure

CHF-6366 Chemical Structure

CAS No. : 1615208-41-7

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CHF-6366 相关抗体

Top Publications Citing Use of Products

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

查看 Calcium Channel 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[1].

IC50 & Target

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

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
分子量

764.87

Formula

C42H48N6O8
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CHF-6366 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

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

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产品名称：
CHF-6366
目录号：
HY-151198
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