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Delcasertib

(Synonyms: KAI-9803; BMS-875944)

目录号: PL09877

Delcasertib (KAI-9803) 是有效，选择性的 δ 蛋白激酶C (δPKC) 抑制剂。Delcasertib (KAI-9803) 可改善急性心肌梗死动物模型的缺血再灌注损伤。

CAS No. :949100-39-4

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中文名称	Delcasertib
英文名称	Delcasertib
英文别名	DELCASERTIB;5G7N7E908H;Delcasertib [USAN:INN];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-alpha-glutamyl-L-leucylglycyl-L-seryl-L-leucine;L-Cysteinyl-L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L-glutaminyl-L- arginyl-L-arginyl-L-arginine (1-;KAI-9803;BMS-875944;Delcasertib
Cas No.	949100-39-4
分子式	C₁₂₀H₁₉₉N₄₅O₃₄S₂
分子量	2880.28
包装储存	Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year
详情描述	Delcasertib (KAI-9803) 是有效，选择性的 δ 蛋白激酶C (δPKC) 抑制剂。Delcasertib (KAI-9803) 可改善急性心肌梗死动物模型的缺血再灌注损伤。

产品详情

Delcasertib (KAI-9803) 是有效，选择性的 δ 蛋白激酶C (δPKC) 抑制剂。Delcasertib (KAI-9803) 可改善急性心肌梗死动物模型的缺血再灌注损伤。

生物活性

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).

性状

Solid

IC50 & Target[1][2]

δPKC

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.
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.
Delcasertib (KAI-9803) has been studied for the prevention of reperfusion injury in patients undergoing angioplasty after acute myocardial infarction.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year

ClinicalTrial

SequenceShortening

Sequence 1:CYGRKKRRQRRR;Sequence 1:CSFNSYELGSL (Disulfide bridge:Cys1-Cys1’)

参考文献

[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.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (34.72 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Delcasertib

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