1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. Delcasertib hydrochloride

Delcasertib hydrochloride (Synonyms: KAI-9803 hydrochloride; BMS-875944 hydrochloride)

目录号: HY-106262B 纯度: 98.11%
产品使用指南

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

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Delcasertib hydrochloride Chemical Structure

Delcasertib hydrochloride Chemical Structure

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     可免费申领三个不同产品的试用装。

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10 mg ¥9900
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI)[1][2].

IC50 & Target[1]

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[1].

MCE 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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

2916.74

Formula

C120H200ClN45O34S2

Sequence Shortening

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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

H2O : 100 mg/mL (34.28 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3428 mL 1.7142 mL 3.4285 mL
5 mM 0.0686 mL 0.3428 mL 0.6857 mL
10 mM 0.0343 mL 0.1714 mL 0.3428 mL
*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
Delcasertib hydrochloride
目录号:
HY-106262B
需求量: