TCMDC-135051 hydrochloride|西域试剂

TCMDC-135051 hydrochloride,98.30%

产品编号：Bellancom-126323B| 分子式：C₂₉H₃₄ClN₃O₃| 分子量：508.05

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货号	价格	库存与货期
Bellancom-126323B	￥4000.00	杭州北京（现货）
Bellancom-126323B	￥6800.00	杭州北京（现货）
Bellancom-126323B	￥19000.00	杭州北京（现货）
Bellancom-126323B	￥28000.00	杭州北京（现货）

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TCMDC-135051 hydrochloride

产品介绍

TCMDC-135051 hydrochloride 是一种高选择性和有效性的蛋白激酶 PfCLK3 抑制剂，具有低的靶外毒性。TCMDC-135051 hydrochloride 可以防止滋养体到裂殖体的转变，破坏转录并减少向蚊子载体的传播。TCMDC-135051 hydrochloride 具有抗寄生虫活性 (EC₅₀=320 nM)。

生物活性

TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC₅₀=320 nM).

体外研究

TCMDC-135051 hydrochloride shows potent activity against P. berghei sporozoites in a liver invasion and development assay in which the compound shows a pEC₅₀ value of 6.17 (EC₅₀=0.40 μM). The kinase assays using recombinant PvCLK3 (P. vivax) and PbCLK3 (P. berghei) show that TCMDC-135051 hydrochloride has near-equipotent inhibition at these two orthologs, with pIC₅₀ values of 7.47 (IC₅₀=0.033 μM) and 7.86 (IC₅₀=0.013 μM), respectively.

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

体内研究

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (164.02 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9683 mL	9.8416 mL	19.6831 mL
5 mM	0.3937 mL	1.9683 mL	3.9366 mL
10 mM	0.1968 mL	0.9842 mL	1.9683 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)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

参考文献