Delcasertib(KAI-9803)hydrochloride是有效，选择性的δ蛋白激酶C(δPKC)抑制剂。Delcasertib(KAI-9803)hydrochloride可改善急性心肌梗死动物模型的缺血再灌注损伤。
Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI)[1][2].
Delcasertib (KAI-9803) is composed of a selective δ-protein kinase C (δPKC) inhibitor peptide derived from the δV1-1 portion of δPKC (termed "cargo peptide"), conjugated reversibly to the cell-penetrating peptide 11-amino acid, arginine-rich sequence of the HIV type 1 transactivator protein (TAT47-57; termed "carrier peptide") via a disulfide bond[1].
Delcasertib (KAI-9803, a single intraperitoneal injection) in mice results in the selective inhibition of PKC translocation in the liver, kidney, lung, heart, and brain[1].Delcasertib (KAI-9803) administration at the end of ischemia has been found to reduce cardiac damage caused by ischemia-reperfusion in a rat model of acute myocardial infarction[1].Delcasertib (KAI-9803) has been studied for the prevention of reperfusion injury in patients undergoing angioplasty after acute myocardial infarction[2]. Animal Model: Six-week-old male Crl:CD(SD) rats[1]
[1]. Miyaji Y, et al. Distribution of KAI-9803, a novel δ-protein kinase C inhibitor, after intravenous administration to rats. Drug Metab Dispos. 2011 Oct;39(10):1946-53. [2]. Bates E, et al. Intracoronary KAI-9803 as an adjunct to primary percutaneous coronary intervention for acute ST-segment elevation myocardial infarction. Circulation. 2008 Feb 19;117(7):886-96.
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