产品
编 号:F756296
分子式:C28H26N2O4S
分子量:486.58
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规格
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1mg
询价
询价
5mg
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生物活性:
LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research. LPA5 antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
LPA5 antagonist 1 (intraperitoneal injection; 17.8 mg/kg; once) treatment shows good brain exposure in vivo.LPA5 antagonist 1 (intraperitoneal injection; 5.6, 10, and 17.8 mg/kg; once) treatment reduces mechanical allodynia in inflammatory pain model.Animal Model:CFA-induced inflammatory pain model in Sprague-Dawley rats
Dosage:5.6, 10, and 17.8 mg/kg
Administration:Intraperitoneal injection; 5.6, 10, and 17.8 mg/kg; once
Result:Reduced mechanical allodynia in a dose-dependent manner.
Animal Model:Male Sprague-Dawley rats
Dosage:17.8 mg/kg
Administration:Intraperitoneal injection; 17.8 mg/kg; once
Result:Showed brain concentrations of 652 ng/mL, after treatment 30 minutes.

体外研究:
LPA5 antagonist 2 (0-10 μM) inhibits hLPA5 calcium mobilization with an IC50 value of 32 nM.LPA5 antagonist 2 (0-10 μM) shows good target selectivity for LPA5.
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