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  4. GPR34 receptor antagonist 3

GPR34 receptor antagonist 3 (Compound 5e) 是一种 GPR34 拮抗剂，IC50 值为0.680 μM。GPR34 receptor antagonist 3 剂量依赖性地抑制溶血磷脂酰丝氨酸诱导的 ERK1/2 磷酸化，无明显细胞毒性。GPR34 receptor antagonist 3 在小鼠神经性疼痛模型中表现出抗感觉活性。

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GPR34 receptor antagonist 3 Chemical Structure

GPR34 receptor antagonist 3 Chemical Structure

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GPR34 receptor antagonist 3 相关抗体

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  • 生物活性

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生物活性

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 [1].

IC50 & Target

IC50:0.680 μM G protein receptor (GPR34) [1]
体外研究
(In Vitro)

GPR34 receptor antagonist 3 (30 μM, 72 h) 在 HEK293T、COS-7、BEAS-2B、Muller、LX-2 和 HUVEC 细胞中没有明显毒性[1]。
GPR34 receptor antagonist 3 (3, 10 and 30 μM, 72 h) 剂量依赖性地抑制表达 GPR34 的 CHO 细胞中 LysoPS 诱导的细胞外信号调节激酶 1/2 (ERK1/2) 的磷酸化[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GPR34 receptor antagonist 3 相关抗体:

Western Blot Analysis[1]

Cell Line: CHO
Concentration: 3,10 and 30 μM
Incubation Time: 72 h
Result: Dose-dependently inhibited the phosphorylation of extracellular signal-regulated kinase1/2 (ERK1/2) induced by LysoPS in CHO cells expressing GPR34.

Cell Viability Assay[1]

Cell Line: HEK293T、COS-7、BEAS-2B、Muller、LX-2 and HUVEC
Concentration: 30 μM
Incubation Time: 72 h
Result: Did not show obvious cytotoxicity against these cell lines with IC50 > 30 μM.
体内研究
(In Vivo)

GPR34 receptor antagonist 3 (200 mg/kg, Intraperitoneal injection,twice a day) 在急性毒性实验中,观察到 C57BL/6J 小鼠死亡, GPR34 receptor antagonist 3 (100 mg/kg, Intraperitoneal injection,twice a day) 在重复毒性实验中,小鼠没有损伤，剂量安全[1]。
GPR34 receptor antagonist 3 (10 or 20 mg/kg, Intraperitoneal injection,twice a day) 在小鼠神经性疼痛模型中可以显著减少机械异常性疼痛[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Neuropathic pain mice model[1]
Dosage: 10 or 20 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reduced mechanical pain in a mouse neuropathic pain model
Animal Model: Oxicity mice model[1]
Dosage: 200 or 100 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Indicated 100 mg/kg was a safe dosage.
分子量

515.98

Formula

C30H26ClNO5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GPR34 receptor antagonist 3 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GPR34 receptor antagonist 3OthersGRP34AntagonistCHOMouseERK1/2Animal model of neuropathic painInhibitorinhibitorinhibit

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