Delcasertib hydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

KAI-9803 hydrochloride
BMS-875944 hydrochloride

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。

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].

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].

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

性状

Solid

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (17.14 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。