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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-GPR37L1 agonist P06
GPR37L1 agonist P06

Chemical Structure : GPR37L1 agonist P06

CAS No.: 1057744-37-2

GPR37L1 agonist P06

货号: PC-27817Not For Human Use, Lab Use Only.

GPR37L1 agonist P06 is a potent, small-molecule agonist of G protein-coupled receptor GPR37-like 1 (GPR37L1), induces dose-dependent potassium influx with EC50 of 182.4 nM in thallium (Tl+) influx assay using HEK293 cells expressing GPR37L1 and the KCNJ3 channel, exhibits significant analgesic effects.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GPR37L1 agonist P06 is a potent, small-molecule agonist of G protein-coupled receptor GPR37-like 1 (GPR37L1), induces dose-dependent potassium influx with EC50 of 182.4 nM in thallium (Tl+) influx assay using HEK293 cells expressing GPR37L1 and the KCNJ3 channel, exhibits significant analgesic effects.
P06 exhibits the strong predicted binding affinity (ΔG = −9.94 kcal/mol).
P06 mitigates PTX-induced mechanical allodynia without affecting motor function.
P06 activates GPR37L1 and preferentially signals through the Gβγ pathway to modulate ion channel function.
P06 (3.6 μg) alleviates mechanical allodynia in the spared nerve injury (SNI) model.
P06 reduces nerve injury–induced SGC and macrophage activation in dorsal root ganglia.
P06 regulates IL-1β release and potassium homeostasis in mouse and human SGC cultures.
GPR37L1 is a glia-selective receptor expressed in astrocytes and satellite glial cells (SGCs), and GPR37L1 protects against the development of neuropathic pain.
GPR37L1 regulates the function of inwardly rectifying potassium channels (e.g., Kir4.1) in SGCs.

物理化学性质&存储条件

分子量 427.45
分子式 C21H18FN3O4S
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

3-acetamido-N-(2-(5-(4-fluorobenzylidene)-2,4-dioxothiazolidin-3-yl)ethyl)benzamide

参考文献

1. Chandra S, et al. Pain. 2026 Sep 1;167(9):2087-2103.

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