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首页-小分子抑制剂&激动剂-GPCR-Sigma Receptor-CM-398
CM-398

Chemical Structure : CM-398

CAS No.: 1121931-70-1

CM-398 (CM398)

货号: PC-21109Not For Human Use, Lab Use Only.

CM-398 (CM398) is a potent, highly selective sigma-2 receptor (σ2R) ligand with Ki of 0.43 nM, >1000-fold selective over σ1R, produces antinociception and anti-allodynia effects.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CM-398 (CM398) is a potent, highly selective sigma-2 receptor (σ2R) ligand with Ki of 0.43 nM, >1000-fold selective over σ1R, produces antinociception and anti-allodynia effects.
CM398 showed promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.
CM-398 dose-dependently (10-45 mg/kg i.p.) reduced mechanical allodynia in the CCI neuropathic pain model, equivalent at the higher dose to the effect of the control analgesic gabapentin (50 mg/kg i.p.).
M-398 dose-dependently produced antinociception in the acetic acid writhing test (ED50 (and 95% C.I.) = 14.7 (10.6–20) mg/kg, i.p.) and the formalin assay (ED50 (and 95% C.I.) = 0.86 (0.44–1.81) mg/kg, i.p.) but was without effect in the 55 °C warm-water tail-withdrawal assay.

物理化学性质&存储条件

分子量 395.50
分子式 C23H29N3O3
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

1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1h)-yl)butyl)-3-methyl-1h-benzo[d]imidazol-2(3H)-one

参考文献

1. Intagliata S., et al. AAPS J. 2020;22:94.

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