Delcasertib (KAI-9803)
(Synonyms: BMS-875944) 目录号 : GC32466
Delcasertib (KAI-9803) (KAI-9803) 是一种有效的选择性 δ-蛋白激酶 C (δPKC) 抑制剂。
Cas No.:949100-39-4
Sample solution is provided at 25 µL, 10mM.
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Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.
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].
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].
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.
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Animal experiment: |
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]. |
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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. |
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| Cas No. | 949100-39-4 | SDF | |
| 别名 | BMS-875944 | ||
| 分子式 | C180H199N45O34S2 | 分子量 | 2880.28 |
| 溶解度 | DMSO : ≥ 100 mg/mL (34.72 mM) | 储存条件 | Store at -20° C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.3472 mL | 1.7359 mL | 3.4719 mL |
| 5 mM | 0.0694 mL | 0.3472 mL | 0.6944 mL |
| 10 mM | 0.0347 mL | 0.1736 mL | 0.3472 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet