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    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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Custom Peptide Synthesis

Delcasertib hydrochloride Chemical Structure

Delcasertib hydrochloride Chemical Structure

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Description

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

 

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, 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].

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.
Molecular Weight

2916.74

Formula

C₁₂₀H₂₀₀ClN₄₅O₃₄S₂

Sequence Shortening

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Protect from light
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
References
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The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

DelcasertibKAI-9803BMS-875944KAI9803KAI 9803BMS875944BMS 875944PKCProtein kinase CacutemyocardialinfarctionischemiaInhibitorinhibitorinhibit

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