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GPR34 receptor antagonist 3

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Catalog No. T82264

Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1/2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].

GPR34 receptor antagonist 3

GPR34 receptor antagonist 3

😃Good
Catalog No. T82264
Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1/2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].
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1 mg$1297-10 days
5 mg$3227-10 days
10 mg$5177-10 days
25 mg$9877-10 days
50 mg$1,6307-10 days
100 mg$2,2207-10 days
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Product Introduction

Bioactivity
Description
Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1/2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].
In vitro
GPR34 receptor antagonist 3, at a concentration of 30 μM administered for 72 hours, exhibited no significant toxicity in HEK293T, COS-7, BEAS-2B, Muller, LX-2, and HUVEC cell lines [1].
In vivo
GPR34 receptor antagonist 3 (200 mg/kg, intraperitoneal injection, twice a day) caused mortality in C57BL/6J mice during acute toxicity trials, while a dose of 100 mg/kg (intraperitoneal injection, twice a day) proved safe in repeated dose toxicity studies [1]. Additionally, doses of 10 or 20 mg/kg (intraperitoneal injection, twice a day) significantly reduced mechanical allodynia in a murine model of neuropathic pain [1].
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