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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 | 现货 | |
5 mg | ¥ 1,930 | 现货 | |
10 mg | ¥ 2,830 | 现货 | |
25 mg | ¥ 4,490 | 现货 | |
50 mg | ¥ 5,920 | 现货 | |
100 mg | ¥ 8,160 | 现货 | |
500 mg | ¥ 16,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,970 | 现货 |
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. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 225 mg/mL (477.1 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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