VK-0214
Based on 1 Customer Validation
VK-0214 is an orally effective agonist of the thyroid β receptor (TRβ). VK-0214 reduces the accumulation of very long-chain fatty acids (VLCFA) by activating ABCD2 expression. VK-0214 has the effect of regulating fatty acid metabolism. VK-0214 can serve as a GBM repurposing candidate compound identified through network pharmacology screening. VK-0214 can be used in research related to X-linked adrenoleukodystrophy (X-ALD) and glioblastoma.
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 : 99.87%
- CAS 番号: 852949-30-5
- 分子式: C23H25O5P
- 分子量:412.42
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
体外実験
VK-0214 is identified as a high-impact node in the white matter-associated disease subnetwork of the glioblastoma biomedical feature network (mc_GBPN), with a total normalized centrality score of 4.407, suggesting that it may serve as a potential repurposing candidate compound for glioblastoma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 852949-30-5
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性状 Solid
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分子量 412.42
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分子式 C23H25O5P
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Color White to pink
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SMILES
O=P(O)(COC1=CC(C)=C(CC2=CC=C(C(CC3=CC=CC=C3)=C2)O)C(C)=C1)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (242.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. 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)
体内:
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: ≥ 2.5 mg/mL (6.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
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.
プロトコル
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. McGowan E, Sanjak J, Mathé EA, Zhu Q. Integrative Rare Disease Biomedical Profile based Network Supporting Drug Repurposing, a case study of Glioblastoma. Res Sq [Preprint]. 2023 Apr 18:rs.3.rs-2809689. doi: 10.21203/rs.3.rs-2809689/v1. Update in: Orphanet J Rare Dis. 2023 Sep 25;18(1):301. [Content Brief]
[2]. McGowan DC, et al. SMALL-MOLECULE AGONISTS OF THYROID HORMONE RECEPTOR BETA (THR-β).
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. 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 | 2.4247 mL | 12.1236 mL | 24.2471 mL | 60.6178 mL |
| 5 mM | 0.4849 mL | 2.4247 mL | 4.8494 mL | 12.1236 mL | |
| 10 mM | 0.2425 mL | 1.2124 mL | 2.4247 mL | 6.0618 mL | |
| 15 mM | 0.1616 mL | 0.8082 mL | 1.6165 mL | 4.0412 mL | |
| 20 mM | 0.1212 mL | 0.6062 mL | 1.2124 mL | 3.0309 mL | |
| 25 mM | 0.0970 mL | 0.4849 mL | 0.9699 mL | 2.4247 mL | |
| 30 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0206 mL | |
| 40 mM | 0.0606 mL | 0.3031 mL | 0.6062 mL | 1.5154 mL | |
| 50 mM | 0.0485 mL | 0.2425 mL | 0.4849 mL | 1.2124 mL | |
| 60 mM | 0.0404 mL | 0.2021 mL | 0.4041 mL | 1.0103 mL | |
| 80 mM | 0.0303 mL | 0.1515 mL | 0.3031 mL | 0.7577 mL | |
| 100 mM | 0.0242 mL | 0.1212 mL | 0.2425 mL | 0.6062 mL |