GPR34 receptor antagonist 3

CAS: F: C30H26ClNO5 W: 515.98

GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist

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Bioactivity	GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model [1].
Target	IC50:0.680 μM G protein receptor (GPR34)
Invitro	GPR34 receptor antagonist 3 (30 μM, 72 h) 在 HEK293T、COS-7、BEAS-2B、Muller、LX-2 和 HUVEC 细胞中没有明显毒性[1]。GPR34 receptor antagonist 3 (3, 10 and 30 μM, 72 h) 剂量依赖性地抑制表达 GPR34 的 CHO 细胞中 LysoPS 诱导的细胞外信号调节激酶 1/2 (ERK1/2) 的磷酸化[1]。 0 --> GPR34 receptor antagonist 3 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	GPR34 receptor antagonist 3 (200 mg/kg, Intraperitoneal injection,twice a day) 在急性毒性实验中,观察到 C57BL/6J 小鼠死亡, GPR34 receptor antagonist 3 (100 mg/kg, Intraperitoneal injection,twice a day) 在重复毒性实验中,小鼠没有损伤，剂量安全[1]。GPR34 receptor antagonist 3 (10 or 20 mg/kg, Intraperitoneal injection,twice a day) 在小鼠神经性疼痛模型中可以显著减少机械异常性疼痛[1]。 Animal Model:
Name	GPR34 receptor antagonist 3
Formula	C30H26ClNO5
Molar Mass	515.98
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Zhou P et al. Discovery of (S)-3-(4-(benzyloxy)phenyl)-2-(2-phenoxyacetamido)propanoic acid derivatives as a new class of GPR34 antagonists. Bioorg Med Chem Lett. 2023 Nov 8:129548.