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TCMDC-135051 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 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 具有抗寄生虫活性 (EC50=320 nM)。

TCMDC-135051 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 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 具有抗寄生虫活性 (EC50=320 nM)。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 792 | In stock | |
| 5 mg | ¥ 1,820 | In stock | |
| 10 mg | ¥ 2,830 | In stock | |
| 25 mg | ¥ 4,490 | In stock | |
| 50 mg | ¥ 5,920 | In stock | |
| 100 mg | ¥ 8,160 | In stock | |
| 200 mg | ¥ 10,900 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,970 | In stock |
TCMDC-135051 相关产品
| 产品描述 | TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector. |
| 体外活性 | In a liver invasion and development assay, TCMDC-135051 shows potent activity against P. berghei sporozoites 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 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[1]. |
| 分子量 | 471.59 |
| 分子式 | C29H33N3O3 |
| CAS No. | 2413716-15-9 |
| Smiles | CCN(CC)Cc1ccc(OC)c(c1)-c1cc2c(ccnc2[nH]1)-c1ccc(C(O)=O)c(c1)C(C)C |
| 密度 | 1.173 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 225 mg/mL (477.1 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.6 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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