
LPA1 receptor antagonist 1
CAS No. 1396006-71-5
LPA1 receptor antagonist 1 ( —— )
产品货号. M33412 CAS No. 1396006-71-5
LPA1 receptor antagonist 1 是具有高度选择性的,溶血磷脂酸 (LPA1) 受体的一个拮抗剂,其 IC50 值为 25 nM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥1899 | 有现货 |
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5MG | ¥2964 | 有现货 |
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10MG | ¥4740 | 有现货 |
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25MG | ¥7187 | 有现货 |
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50MG | ¥9619 | 有现货 |
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100MG | ¥12776 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称LPA1 receptor antagonist 1
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述LPA1 receptor antagonist 1 是具有高度选择性的,溶血磷脂酸 (LPA1) 受体的一个拮抗剂,其 IC50 值为 25 nM。
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产品描述LPA1 receptor antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.
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体外实验LPA1 receptor antagonist 1 (compound 2) displays very potent and highly selective inhibitory activity toward LPA1, with little inhibition on LPA3 even at very high concentrations. To our knowledge, LPA1 receptor antagonist 1 is the most selective nonlipid LPA1 antagonist so far reported. It appears that compounds (e.g., LPA1 receptor antagonist 1) from the N-aryltriazole chemical class are much more selective for LPA1 than compounds from the corresponding pyrazole series. In comparison with Ki16425 and AM095, LPA1 receptor antagonist 1 shows much improved antiproliferative activity. LPA1 receptor antagonist 1 demonstrates the highest LPA1 selectivity and attenuated LPA-induced NHLF proliferation and contraction with high potency.
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体内实验Oral dosing of LPA1 receptor antagonist 1 in mice causes a dose-dependent reduction in serum histamine levels induced following intravenous LPA stimulation. When mice are orally dosed with LPA1 antagonist 1 (100 mg/kg, aqueous suspension) prior to intravenous LPA injection, the LPA-induced histamine level is significantly blocked A clear PK/PD relationship is demonstrated by the correlation between the levels of LPA1 receptor antagonist 1 and LPA-induced histamine concentrations in plasma. Although AM095 almost completely blocks histamine release (100 mg/kg), analysis of plasma samples revealed more than 65-fold higher concentrations of AM095 than LPA1 receptor antagonist 1 (100 mg/kg). The ability of LPA1 receptor antagonist 1 to block histamine release at much lower plasma concentration suggests that further improvement of pharmacokinetic properties of this chemical class could lower the effective dose.
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同义词——
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通路GPCR/G Protein
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靶点LPA Receptor
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受体LPA Receptor
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研究领域——
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适应症——
化学信息
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CAS Number1396006-71-5
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分子量482.53
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分子式C28H26N4O4
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纯度>98% (HPLC)
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溶解度——
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SMILESC(O)(=O)C1(CC1)C2=CC=C(C=C2)C3=CC=C(C=C3)N4C(NC(O[C@H](C)C5=CC=CC=C5)=O)=C(C)N=N4
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Qian Y, et al. Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts. J Med Chem. 2012 Sep 13;55(17):7920-39.?
产品手册




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