到目前為止,已經鑒定出六種類型的受體LPA 1 -6,它們負責LPA的大部分生物活性。近年來對小鼠基因靶向和這些受體家族疾病的研究表明,LPA參與了多種病理生理狀態(tài)。LPA拮抗劑已經引起了相當大的關注,并且已經報道了許多具有LPA拮抗活性的小分子。Ki 16425是LPA 1和LPA 3受體的拮抗劑,對LPA 2具有中等活性。參考文獻:由Bioz提供技術支持查看Bioz 1的更多詳情。Hideo Ohta et al“Ki16425 a Subtype-Selective Antagonist for EDG-Family Lysophosphatidic Acid Receptors” Molecular Pharmacology 2003 166(4)994-10052. Jing Zhao et al“溶血磷脂酸受體1拮抗劑Ki 16425在腹膜膿毒癥小鼠模型中阻斷腹部和全身炎癥”轉化研究2015 166(1)80 - 88?
產品描述
To date six types of receptors LPA1-6 have been identified and are responsible for most of the biological activities of LPA. Recent studies on gene targeting in mice and family diseases of these receptors revealed that LPA is involved in various patho-physiological states. LPA antagonists have attracted considerable attention and numerous small molcules having LPA antagonistic activity have been reported. Ki16425 is an antagonist of LPA1 and LPA3 receptors with moderate activity against LPA2.References: Powered by Bioz See more details on Bioz1. Hideo Ohta et al a€?Ki16425 a Subtype-Selective Antagonist for EDG-Family Lysophosphatidic Acid Receptorsa€? Molecular Pharmacology 2003 166(4) 994-10052. Jing Zhao et al a€?Lysophosphatidic Acid Receptor 1 antagonist Ki16425 Blunts Abdominal and Systemic Inflammation in a Mouse Model of Peritoneal Sepsisa€? Translational Research 2015 166(1) 80a€“88