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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-BPRMU191
BPRMU191

Chemical Structure : BPRMU191

CAS No.: 2131199-52-3

BPRMU191 (BPRMU-191)

货号: PC-22776Not For Human Use, Lab Use Only.

BPRMU191 is a unique mu-opioid receptor (MOR) modulator with EC50 of 2.17 uM in FLIPR Ca2+ assay using CHO-K1/MOR/Gα15 cells, BPRMU191 binds to MOR in the presence of naloxone.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BPRMU191 is a unique mu-opioid receptor (MOR) modulator with EC50 of 2.17 uM in FLIPR Ca2+ assay using CHO-K1/MOR/Gα15 cells, BPRMU191 binds to MOR in the presence of naloxone.
BPRMU191 interacts with ECL2 (extracellular loop 2) of MOR.
BPRMU191 exemplifies an antagonist-to-agonist modulator of mu-opioid receptor (MOR).
BPRMU191 converts opioid antagonists to G protein-biased agonists of MOR.
Co-application of BPRMU191 and morphinan antagonists resulted in MOR-dependent analgesia with diminished side effects, including gastrointestinal dysfunction, antinociceptive tolerance, and physical and psychological dependence.
BPRMU191/naltrexone produces antinociceptive effects in mouse models of clinical pain.

物理化学性质&存储条件

分子量 331.36
分子式 C17H14FNO3S
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

4-(2-(4-fluorophenyl)-4-oxothiazolidin-3-yl)-3-methylbenzoic acid

参考文献

1. Huang YH, et al. Cell Chem Biol. 2024 Jul 9:S2451-9456(24)00272-1.

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