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VU 0134992 是一个亚型偏好的,口服有效的和选择性的内向整流钾通道 Kir4.1阻滞剂,IC50为 0.97 μM。在 -120 mV 时,VU0134992对同分 Kir4.1 比 Kir4.1/5.1 共分通道 (IC50=9 μM) 高出 9 倍的选择性。
VU 0134992 是一个亚型偏好的,口服有效的和选择性的内向整流钾通道 Kir4.1阻滞剂,IC50为 0.97 μM。在 -120 mV 时,VU0134992对同分 Kir4.1 比 Kir4.1/5.1 共分通道 (IC50=9 μM) 高出 9 倍的选择性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 666 | 现货 | |
5 mg | ¥ 1,360 | 现货 | |
10 mg | ¥ 2,030 | 现货 | |
25 mg | ¥ 3,330 | 现货 | |
50 mg | ¥ 4,660 | 现货 | |
100 mg | ¥ 5,920 | 现货 | |
200 mg | ¥ 8,160 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,510 | 现货 |
产品描述 | VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM |
靶点活性 | KIR4.1:0.97 µM |
体外活性 | VU0134992 inhibits Kir4.1 with an IC50 value of 0.97 μM and is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50 = 9 μM) at -120 mV.?In thallium (Tl+) flux assays, VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2;?is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1;?and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2. |
体内活性 | VU0134992 displayed a large free unbound fraction (fu) in rat plasma (fu = 0.213).?Consistent with the known role of Kir4.1 in renal function, oral dosing of VU0134992 led to a dose-dependent diuresis, natriuresis, and kaliuresis in rats. |
别名 | VU 0134992 |
分子量 | 411.38 |
分子式 | C20H31BrN2O2 |
CAS No. | 755002-90-5 |
Smiles | N(C(COC1=C(Br)C=C(C(C)C)C=C1)=O)C2CC(C)(C)NC(C)(C)C2 |
密度 | no data available |
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: 60 mg/ml (145.85 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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