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编 号:F535252
分子式:C120H199N45O34S2
分子量:2880.28
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生物活性:
Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).

体内研究:
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.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.Delcasertib (KAI-9803) has been studied for the prevention of reperfusion injury in patients undergoing angioplasty after acute myocardial infarction.Animal Model:Six-week-old male Crl:CD(SD) rats.
Dosage:1 mg/kg (Pharmacokinetic Analysis).
Administration:Via the femoral vein.
Result:The distribution to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47-57.

体外研究:
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.
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