1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. Propylbenzilylcholine mustard

Propylbenzilylcholine mustard (PrBCM) 是一种针对大鼠心脏毒蕈碱受体的不可逆性、共价结合型选择性拮抗剂,优先靶向对激动剂呈低亲和力的毒蕈碱受体亚型。Propylbenzilylcholine mustard 可在体外以剂量和时间依赖的方式灭活该类受体,其受体选择性在不同离子强度及含GTP的缓冲体系中均能稳定保持。Propylbenzilylcholine mustard 可应用于毒蕈碱受体结构与功能的基础药理学研究,尤其聚焦于心脏毒蕈碱受体异质性及相关心血管药理学研究。

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Propylbenzilylcholine mustard

Propylbenzilylcholine mustard Chemical Structure

CAS No. : 36167-80-3

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生物活性

Propylbenzilylcholine mustard (PrBCM) is an irreversible, covalently binding selective antagonist targeting rat cardiac muscarinic receptors, with a preference for muscarinic receptor subtypes that show low affinity for agonists. Propylbenzilylcholine mustard inactivates such receptors in a dose- and time-dependent manner in vitro, and its receptor selectivity remains stable across different ionic strengths and in GTP-containing buffer systems. Propylbenzilylcholine mustard can be applied to basic pharmacological studies on the structure and function of muscarinic receptors, especially focusing on the heterogeneity of cardiac muscarinic receptors and related cardiovascular pharmacological research[1].

体外研究
(In Vitro)

Propylbenzilylcholine mustard (3-10 nM; 0-40 min; 25 °C) 可使大鼠心脏毒蕈碱受体失活:在 3 nM 时该过程符合一级动力学,而在 10 nM 时失活速率随时间减慢[1]
Propylbenzilylcholine mustard (1-10 nM; 5 min; 25 °C) 可选择性灭活大鼠心脏中具有低激动剂亲和力的毒蕈碱受体;即使在总[3H]-NMS 标记的受体被灭活 50%后,仍有高达 90%的具有高激动剂亲和力的[3H]-oxo-M 标记受体保持完整[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

375.89

Formula

C21H26ClNO3

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Propylbenzilylcholine mustard
目录号:
HY-186083
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