TNP
Based on 1 Customer Validation
TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC50s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].
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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: 98.04%
- CAS 番号: 519178-28-0
- 分子式: C20H16F3N7O2
- 分子量:443.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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: 0.55 µM (IP6K1), 10.2 μM (IP3K)[1].
TNP (10 μM; 4 h) significantly reduces IP7 levels and activates Akt phosphorylation in HCT116 cells, enhancing insulin sensitivity via IP6K inhibition[1]. TNP (100 nM; 10 min) inhibits recombinant CYP3A4 activity (IC??≈149 nM) in a concentration-dependent competitive binding manner[2].
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.
化学情報
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CAS 番号 519178-28-0
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性状 Solid
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分子量 443.38
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分子式 C20H16F3N7O2
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Color Light yellow to yellow
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SMILES
FC(C1=CC(CNC2=NC(NCC3=CC=C([N+]([O-])=O)C=C3)=C4N=CNC4=N2)=CC=C1)(F)F
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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 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 37.5 mg/mL (84.58 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: 3.75 mg/mL (8.46 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 3.75 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: 3.75 mg/mL (8.46 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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.
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.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (479 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chang YT, et al. Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. Chembiochem. 2002 Sep 2;3(9):897-901. [Content Brief]
[2]. Ghoshal S, et al. TNP [N2-(m-Trifluorobenzyl), N6-(p-nitrobenzyl)purine] ameliorates diet induced obesity and insulin resistance via inhibition of the IP6K1 pathway. Mol Metab. 2016 Aug 21;5(10):903-917. [Content Brief]
[3]. Lee S, et al. TNP and its analogs: Modulation of IP6K and CYP3A4 inhibition. J Enzyme Inhib Med Chem. 2022 Dec;37(1):269-279. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2554 mL | 11.2770 mL | 22.5540 mL | 56.3850 mL |
| 5 mM | 0.4511 mL | 2.2554 mL | 4.5108 mL | 11.2770 mL | |
| 10 mM | 0.2255 mL | 1.1277 mL | 2.2554 mL | 5.6385 mL | |
| 15 mM | 0.1504 mL | 0.7518 mL | 1.5036 mL | 3.7590 mL | |
| 20 mM | 0.1128 mL | 0.5639 mL | 1.1277 mL | 2.8193 mL | |
| 25 mM | 0.0902 mL | 0.4511 mL | 0.9022 mL | 2.2554 mL | |
| 30 mM | 0.0752 mL | 0.3759 mL | 0.7518 mL | 1.8795 mL | |
| 40 mM | 0.0564 mL | 0.2819 mL | 0.5639 mL | 1.4096 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4511 mL | 1.1277 mL | |
| 60 mM | 0.0376 mL | 0.1880 mL | 0.3759 mL | 0.9398 mL | |
| 80 mM | 0.0282 mL | 0.1410 mL | 0.2819 mL | 0.7048 mL |
TNP 関連分類
HY-110079 関連分類
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