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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-CIM0216
CIM0216

Chemical Structure : CIM0216

CAS No.: 1031496-06-6

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CIM0216 (CIM-0216)

货号: PC-24729Not For Human Use, Lab Use Only.

CIM0216 is a potent, selective synthetic TRPM3 activator / agonist, evokes robust increases in intracellular Ca2+ concentration in HEK-TRPM3 cells with EC50 of 0.77 uM.

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5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CIM0216 is a potent, selective synthetic TRPM3 activator / agonist, evokes robust increases in intracellular Ca2+ concentration in HEK-TRPM3 cells with EC50 of 0.77 uM.
CIM0216 exceeds the potency and apparent affinity of canonical TRPM3 agonist, pregnenolone sulfate (PS) (EC50=3.0 uM).
CIM0216 (10 uM) has no stimulating/blocking effect on TRPM1, TRPM4, TRPM6, or TRPM7 currents, and weak activity against TRPM2 (16.6% block) and TRPM5 (33.5% block).
CIM0216 modualtes PS-induced TRPM3 currents with EC50 of 42 nM in HEK-TRPM3 cells.
CIM0216 evoked robust calcium influx in TRPM3-expressing somatosensory neurons, and intradermal injection of the compound induced a TRPM3-dependent nocifensive behavior.
CIM0216 elicited the release of the peptides calcitonin gene-related peptide (CGRP) from sensory nerve terminals and insulin from isolated pancreatic islets in a TRPM3-dependent manner.

物理化学性质&存储条件

分子量 347.42
分子式 C21H21N3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(3,4-Dihydroquinolin-1(2H)-yl)-N-(5-methylisoxazol-3-yl)-2-phenylacetamide

参考文献

1. Held K, et al. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):E1363-72.

2. Rubil S, et al. Channels (Austin). 2017 Jan 2;11(1):79-83.

3. Vangeel L, et al. Br J Pharmacol. 2020 Jun;177(12):2683-2695.

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