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VTX-27 是蛋白激酶 C θ (PKC θ) 的一种选择性抑制剂,对 PKC θ 和 PKC δ 的 Ki 值分别为 0.08 nM 和 16 nM。
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VTX-27 是蛋白激酶 C θ (PKC θ) 的一种选择性抑制剂,对 PKC θ 和 PKC δ 的 Ki 值分别为 0.08 nM 和 16 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 756 | 现货 | |
2 mg | ¥ 1,120 | 现货 | |
5 mg | ¥ 2,220 | 现货 | |
10 mg | ¥ 3,190 | 现货 | |
25 mg | ¥ 4,960 | 现货 | |
50 mg | ¥ 6,700 | 现货 | |
100 mg | ¥ 8,880 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,980 | 现货 |
产品描述 | VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ). |
靶点活性 | PKCθ:0.08 nM (ki), PKCδ:16 nM (ki), PKCα:356 nM (ki) |
体外活性 | It has also been found that VTX-27 has good selectivity to other PKC family members, especially the classic isoforms (except for PKCβI, >1000 times, 200 times) and atypical isoforms (>10000 times). As expected, it is more challenging to obtain selectivity for more closely related novel PKC family members, which is 200 times more selective than PKCδ. |
体内活性 | VTX-27 shows the best PK profile with low clearance (7 mL/min/kg), good oral bioavailability (65%), and long half-life (4.7 h). A single dose of VTX-27 is administered orally at 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL) and demonstrates potent dose-dependent inhibition of IL-2 production. |
分子量 | 418.9 |
分子式 | C20H24ClFN6O |
CAS No. | 1321924-70-2 |
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: 125 mg/mL (298.40 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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