| Description | Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC). |
| In vitro | Delcasertib由选择性δ-蛋白激酶C(δPKC)抑制剂肽组成，该肽源自δPKC的δV1-1部分(称为“货载肽”)，通过一个二硫键可逆地连接到细胞穿透肽11个氨基酸、富含精氨酸的HIV-1型激活蛋白(TAT47-57; 称为“载体肽”)。 |
| In vivo | KAI-9803 在急性心肌梗塞中通过特异性调节PKC delta或epsilon的膜转移缓解病理状况，并减少疼痛。Delcasertib通过在进行初级经皮冠状动脉介入治疗的ST段抬高型心肌梗塞时，经冠状动脉内注射给药，表现出可接受的安全性和耐受性。在缺血末期进行Delcasertib治疗，已被发现能减少大鼠急性心肌梗塞模型中由缺血-再灌注引起的心脏损伤。14C-KAI-9803能迅速被多种组织吸收，包括心脏（1.21 μg eq/g组织），同时又能快速从全身循环中清除。Delcasertib通过可逆的与TAT47–57结合，促进了其向肝、肾和心脏等组织的分布。 |
| Synonyms | KAI-9803, BMS-875944 |
| molecular weight | 2880.28 |
| Molecular formula | C120H199N45O34S2 |
| CAS | 949100-39-4 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 99 mg/mL(34.37 mM) |
| References | 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. |