949100-39-4
949100-39-4 structure
- Name: KAI-9803
- Chemical Name: KAI-9803
- CAS Number: 949100-39-4
- Molecular Formula: C120H199N45O34S2
- Molecular Weight: 2880.28
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2018-05-19 16:21:37
- Modify Date: 2024-01-14 16:27:15
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Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.
| Name | KAI-9803 |
|---|
| Description | Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. |
|---|---|
| Related Catalog | |
| Target |
δPKC |
| In Vitro | 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]. |
| In Vivo | 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. 14C-KAI-9803 is rapidly delivered to many tissues, including the heart (1.21 μg eq/g tissue), while being quickly cleared from the systemic circulation. The distribution of Delcasertib (KAI-9803) to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47–57[1]. KAI-9803 ameliorates pathological conditions in acute myocardial infarction and reduce pain via specific modulation of membrane-translocation of PKC delta or epsilon. Delcasertib (KAI-9803) has an acceptable safety and tolerability profile when delivered via intracoronary injection during primary percutaneous coronary intervention for ST-segment elevation myocardial infarction[2]. |
| Animal Admin | Rats[1] For pharmacokinetic studies, 14Delcasertib (KAI-9803) (1 mg/kg) is administered to Six-week-old male Crl:CD(SD) rats via the femoral vein and approximately 0.2 mL of blood is collected from the jugular vein at 1, 2, 5, 10, and 15 min postdose with a heparinized syringe containing 10 μL of 400 mM diisopropylfluorophosphate dissolved in acetonitrile to prevent rapid degradation of the peptide. The radioactivity in the blood and plasma samples is measured using a liquid scintillation counter[1]. |
| References |
| Molecular Formula | C120H199N45O34S2 |
|---|---|
| Molecular Weight | 2880.28 |