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GPR34 receptor antagonist 3

Catalog No.GC71335

GPR34 receptor antagonist 3 (화합물 5e) 는 IC50이 0.680 μM인 GRP34 옹색제 종류입니다.

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GPR34 receptor antagonist 3 Chemical Structure

Size 가격 재고 수량
1 mg
US$140.00
재고 있음
5 mg
US$351.00
재고 있음
10 mg
US$563.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
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 .

GPR34 receptor antagonist 3 (30 μM, 72 h) in HEK293T, COS-7, BEAS-2B, Muller, LX-2 and HUVEC cells do not show obvious cytotoxicity against these cell lines with IC50 > 30 μM[1].
GPR34 receptor antagonist 3 (3, 10 and 30 μM, 72 h) dose-dependently inhibited the phosphorylation of extracellular signal-regulated kinase1/2 (ERK1/2) induced by LysoPS in CHO cells expressing GPR34[1].

GPR34 receptor antagonist 3 (200 mg/kg, Intraperitoneal injection, twice a day) observes the death of C57BL/6J mice in the acute toxicity experiment, GPR34 receptor antagonist 3 (100 mg/kg, Intraperitoneal injection, twice a day) mice has no damage during repeated toxicity experiment, and the dose was safe [1].
GPR34 receptor antagonist 3 (10 or 20 mg/kg, Intraperitoneal injection,twice a day) can significantly reduce mechanical pain in a mouse neuropathic pain model [1].

References:
[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.

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