| Identification | Back Directory | [Name]
Delcasertib | [CAS]
949100-39-4 | [Synonyms]
KAI-9803
BMS-875944
Delcasertib
BMS875944,Inhibitor,BMS 875944,KAI 9803,Delcasertib,inhibit,Protein kinase C,PKC,KAI9803
L-Arginine, L-cysteinyl-L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L-glutaminyl-L-arginyl-L-arginyl-, (1→1')-disulfide with L-cysteinyl-L-seryl-L-phenylalanyl-L-asparaginyl-L-seryl-L-tyrosyl-L-α-glutamyl-L-leucylglycyl-L-seryl-L-leucine | [Molecular Formula]
C120H199N45O34S2 | [MDL Number]
MFCD31657352 | [MOL File]
949100-39-4.mol | [Molecular Weight]
2880.31 |
| Chemical Properties | Back Directory | [density ]
1.54±0.1 g/cm3(Predicted) | [solubility ]
DMSO:100.0(Max Conc. mg/mL);34.72(Max Conc. mM) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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)[1][2]. | [in vivo]
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]. | | 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.
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| [IC 50]
δPKC | [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. DOI:10.1124/dmd.111.040725
[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. DOI:10.1161/CIRCULATIONAHA.107.759167 |
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| Company Name: |
ChemeGen
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
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