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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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥1899 有现货
5MG ¥2964 有现货
10MG ¥4740 有现货
25MG ¥7187 有现货
50MG ¥9619 有现货
100MG ¥12776 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    LPA1 receptor antagonist 1
  • 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
  • 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。
  • 产品描述
    LPA1 receptor antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.
  • 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.
  • 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.
  • 同义词
    ——
  • 通路
    GPCR/G Protein
  • 靶点
    LPA Receptor
  • 受体
    LPA Receptor
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1396006-71-5
  • 分子量
    482.53
  • 分子式
    C28H26N4O4
  • 纯度
    >98% (HPLC)
  • 溶解度
    ——
  • SMILES
    C(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
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 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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