Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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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) resulted in mortality in C57BL/6J mice during acute toxicity trials, whereas GPR34 receptor antagonist 3 (100 mg/kg, intraperitoneal injection, twice a day) demonstrated no harm and was deemed safe in repeated dose toxicity studies [1]. Furthermore, at dosages of 10 or 20 mg/kg administered intraperitoneally twice a day, GPR34 receptor antagonist 3 significantly reduced mechanical allodynia in a murine model of neuropathic pain [1]. |
Molecular Weight | N/A |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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GPR34 receptor antagonist 3 inhibitor inhibit