Delcasertib-KAI-9803-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDelcasertibCat. No.: HY-106262CAS No.: 949100-39-4Synonyms: KAI-9803; BMS-875944分式: CHNOS分量: 2880.28作靶點: PKC作通路: Epigenetics; TGF-beta/Smad儲存式: Powder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 1

2、00 mg/mL (34.72 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 0.3472 mL 1.7359 mL 3.4719 mL5 mM 0.0694 mL 0.3472 mL 0.6944 mL10 mM 0.0347 mL 0.1736 mL 0.3472 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?/p>

3、(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 7.69 mg/mL (2.67 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (0.87 mM); Clear solution1/2 Master of Small M

4、olecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (0.87 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Delcasertib (KAI-9803)有效，選擇性的蛋激酶C (PKC) 抑制劑。IC50 & Target PKC體外研究 Delcasertib (KAI-9803) is composed of a selective -protein kinase C (PKC) inhibitor peptide derived f

5、romthe V1-1 portion of PKC (termed “cargo peptide”), conjugated reversibly to the cell-penetrating peptide 11-amino acid, arginine-rich sequence of the HIV type 1 transactivator protein (TAT4757; termed “carrierpeptide”) via a disulfide bond 1.體內(nèi)研究 Delcasertib (KAI-9803) administration at the end of

6、 ischemia has been found to reduce cardiac damagecaused by ischemia-reperfusion in a rat model of acute myocardial infarction. 14C-KAI-9803 is rapidlydelivered to many tissues, including the heart (1.21 g eq/g tissue), while being quickly cleared from thesystemic circulation. The distribution of Del

7、casertib (KAI-9803) to tissues such as the liver, kidney, and heartis facilitated by the reversible conjugation to TAT4757 1. KAI-9803 ameliorates pathological conditions inacute myocardial infarction and reduce pain via specific modulation of membrane-translocation of PKC deltaor epsilon. Delcasert

8、ib (KAI-9803) has an acceptable safety and tolerability profile when delivered viaintracoronary injection during primary percutaneous coronary intervention for ST-segment elevationmyocardial infarction 2.PROTOCOLAnimal Rats 1Administration 1 For pharmacokinetic studies, 14Delcasertib (KAI-9803) (1 m

9、g/kg) is administered to Six-week-old maleCrl:CD(SD) rats via the femoral vein and approximately 0.2 mL of blood is collected from the jugular vein at1, 2, 5, 10, and 15 min postdose with a heparinized syringe containing 10 L of 400 mMdiisopropylfluorophosphate dissolved in acetonitrile to prevent r

10、apid degradation of the peptide. Theradioactivity in the blood and plasma samples is measured using a liquid scintillation counter 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Miyaji Y, et al. Distribution of KAI-9803, a novel -protein

11、 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 elevationmyocardial infarction. Circulation. 2008 Feb 19;117(7):886-96.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has n