VU591
Based on 1 Customer Validation
VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM. VU591 can be used for neurological research with HY-108585 (the equivalent of VU591 hydrochloride).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.81%
- CAS 番号: 1222810-74-3
- 分子式: C16H12N6O5
- 分子量:368.30
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
IC50: 0.24 μM (ROMK)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.24 μM
Compound: 2
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Inhibition of ROMK S44D mutant expressed in HEK293 cells assessed as inhibition of thallium efflux incubated for 20 mins prior to thallium addition measured after 7 to 12 secs by fluorescence assay
Inhibition of ROMK S44D mutant expressed in HEK293 cells assessed as inhibition of thallium efflux incubated for 20 mins prior to thallium addition measured after 7 to 12 secs by fluorescence assay
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[PMID: 24900480] |
| HEK293 | IC50 |
240 nM
Compound: 3; VU591
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Inhibition of rat ROMK1 expressed in HEK293 cells by Tl+ flux assay
Inhibition of rat ROMK1 expressed in HEK293 cells by Tl+ flux assay
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[PMID: 31034224] |
VU591 is a selective ROMK inhibitor and a ROMK channel pore blocker. VU591 can bind serum protein and has high metabolic stability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice[2]
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Dosage:1.842 μg
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Administration:i.c.v.; 1.842 μg;
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Result:Showed antidepressive effect in the tail suspension test (TST).
化学情報
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CAS 番号 1222810-74-3
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性状 Solid
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分子量 368.30
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分子式 C16H12N6O5
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Color Light yellow to yellow
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SMILES
O=[N+]([O-])C1=CC(NC(COCC2=NC3=C(N2)C=C([N+]([O-])=O)C=C3)=N4)=C4C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 62.5 mg/mL (169.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bhave G, et al. Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel. Mol Pharmacol. 2011 Jan;79(1):42-50. [Content Brief]
[2]. Masayoshi Okada, et al. Antidepressive effect of an inward rectifier K+ channel blocker peptide, tertiapin-RQ. PLoS One. 2020 Nov 13;15(11):e0233815. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7152 mL | 13.5759 mL | 27.1518 mL | 67.8794 mL |
| 5 mM | 0.5430 mL | 2.7152 mL | 5.4304 mL | 13.5759 mL | |
| 10 mM | 0.2715 mL | 1.3576 mL | 2.7152 mL | 6.7879 mL | |
| 15 mM | 0.1810 mL | 0.9051 mL | 1.8101 mL | 4.5253 mL | |
| 20 mM | 0.1358 mL | 0.6788 mL | 1.3576 mL | 3.3940 mL | |
| 25 mM | 0.1086 mL | 0.5430 mL | 1.0861 mL | 2.7152 mL | |
| 30 mM | 0.0905 mL | 0.4525 mL | 0.9051 mL | 2.2626 mL | |
| 40 mM | 0.0679 mL | 0.3394 mL | 0.6788 mL | 1.6970 mL | |
| 50 mM | 0.0543 mL | 0.2715 mL | 0.5430 mL | 1.3576 mL | |
| 60 mM | 0.0453 mL | 0.2263 mL | 0.4525 mL | 1.1313 mL | |
| 80 mM | 0.0339 mL | 0.1697 mL | 0.3394 mL | 0.8485 mL | |
| 100 mM | 0.0272 mL | 0.1358 mL | 0.2715 mL | 0.6788 mL |
VU591 関連分類
HY-108585A 関連分類
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