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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].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $129 | 7-10 days | |
5 mg | $322 | 7-10 days | |
10 mg | $517 | 7-10 days | |
25 mg | $987 | 7-10 days | |
50 mg | $1,630 | 7-10 days | |
100 mg | $2,220 | 7-10 days |
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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