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- 文献和实验
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- 保存条件:
4°C, sealed storage, away from moisture
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1052515-91-9
- 规格:
10 mM * 1 mL/5 mg/10 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥770.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥700.0 |
| 规格: | 10 mg | 产品价格: | ¥1250.0 |
| 规格: | 50 mg | 产品价格: | ¥3800.0 |
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VU0134992 hydrochloride
CAS No. : 1052515-91-9
MCE 国际站:VU0134992 hydrochloride
产品活性:VU0134992 hydrochloride 是第一个亚型偏好的,具有口服活性和选择性的内向整流钾通道 Kir4.1 阻滞剂,IC50 值为 0.97 μM。VU0134992 hydrochloride 在 -120 mV 时,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。
研究领域:Membrane Transporter/Ion Channel
作用靶点:Potassium Channel
In Vitro: VU0134992 hydrochloride 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.The selectivity of VU0134992 hydrochloride for Kir4.1 versus nine other members of the Kir channel family was evaluated at concentrations ranging from 0.3 nM to 30 µM in 11-point CRC experiments, using established Tl+ flux assays. VU0134992 hydrochloride inhibits Kir3.1/Kir3.2 (92% inhibition at 30 µM, IC50=2.5 µM), Kir3.1/Kir3.4 (92% inhibition at 30 µM, IC50=3.1 µM), and Kir4.2 (100% inhibition at 30 µM, IC50=8.1 µM) with approximately the same efficacy and potency that VU0134992 inhibits Kir4.1 (100% at 30 µM, IC50=5.2 µM).
In Vivo: VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion.
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文献和实验barriers. Plant Biotechnol. J. 4 , 575-603. 10. Patnaik, D, Vishnudasan, D. and Khurana, P. (2006) Agrobacterium-mediated transformation of matureembryos of T riticu m a estivu m and T riticu m d u ru m . Cu rren t S ci. 91,
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