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LPA1 receptor antagonist 1

CAS No. : 1396006-71-5

MCE 站：LPA1 receptor antagonist 1

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: 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.

In Vivo: 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.

相关产品：Fingolimod hydrochloride  |  PF-543 Citrate  |  Ki16425  |  JTE-013  |  TY-52156  |  AM095  |  Sphingosine-1-phosphate  |  FTY720 (S)-Phosphate  |  SEW?2871  |  LPA2 antagonist 1  |  CYM-5541  |  ONO-7300243  |  1-Oleoyl lysophosphatidic acid  |  AS2717638  |  CYM50308  |  Radioprotectin-1  |  Ceranib-2  |  LPA2 antagonist 2  |  S1P1 Agonist III  |  CYM50260  |  4-Deoxypyridoxine 5'-phosphate  |  GRI977143  |  H2L 5765834  |  Ki16198  |  NSC12404  |  PF-543 hydrochloride  |  S1PR1-MO-1

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