Metoprine
Based on 1 Customer Validation
Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
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- Pureza : 99.67%
- No. CAS: 7761-45-7
- Fòrmula: C11H10Cl2N4
- Peso molecular:269.13
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF S-180 | ED50 |
0.05 μM
Compound: metoprine
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Cytotoxic activity against the S180 cell cultures
Cytotoxic activity against the S180 cell cultures
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[PMID: 6928967] |
| L1210 | ED50 |
0.22 μM
Compound: metoprine
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Cytotoxic activity against the L1210 cell cultures
Cytotoxic activity against the L1210 cell cultures
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[PMID: 6928967] |
| W256 | ED50 |
0.05 μM
Compound: metoprine
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Cytotoxic activity against the Walker 256 carcinosarcoma in rats
Cytotoxic activity against the Walker 256 carcinosarcoma in rats
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[PMID: 6928967] |
In Vivo
Intraperitoneal administration of Metoprine produces various behavioral effects, including decreases in food intake and increases in water consumption[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-dawley rats (200-280g)[2]
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Dosage:2, 5, 10 mg/kg
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Administration:IP
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Result:Ameliorated the memory deficits induced by nucleus basalis magnocellularis (NBM) lesions in a dose-dependent manner and significanty prolonged transfer latency at a high dose of 10 mg/kg.
Chemical Information
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No. CAS 7761-45-7
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Appearance Solid
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Peso molecular 269.13
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Fòrmula C11H10Cl2N4
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Color Off-white to yellow
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SMILES
CC1=C(C(N)=NC(N)=N1)C2=CC=C(C(Cl)=C2)Cl
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Synonyms
BW 197U
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 20.83 mg/mL (77.40 mM; ultrasonic and warming and heat to 60°C; 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. 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (7.73 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.
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Junichi Kitanaka, et al. Brain Histamine N-Methyltransferase As a Possible Target of Treatment for Methamphetamine Overdose. Drug Target Insights. 2016 Mar 2;10:1-7. [Content Brief]
[2]. Zhong Chen, et al. Effects of brain histamine on memory deficit induced by nucleus basalis-lesion in rats. Acta Pharmacol Sin. 2002 Jan;23(1):66-70. [Content Brief]
[3]. John R Horton, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J Mol Biol. 2005 Oct 21;353(2):334-344. [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. 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 | 3.7157 mL | 18.5784 mL | 37.1568 mL | 92.8919 mL |
| 5 mM | 0.7431 mL | 3.7157 mL | 7.4314 mL | 18.5784 mL | |
| 10 mM | 0.3716 mL | 1.8578 mL | 3.7157 mL | 9.2892 mL | |
| 15 mM | 0.2477 mL | 1.2386 mL | 2.4771 mL | 6.1928 mL | |
| 20 mM | 0.1858 mL | 0.9289 mL | 1.8578 mL | 4.6446 mL | |
| 25 mM | 0.1486 mL | 0.7431 mL | 1.4863 mL | 3.7157 mL | |
| 30 mM | 0.1239 mL | 0.6193 mL | 1.2386 mL | 3.0964 mL | |
| 40 mM | 0.0929 mL | 0.4645 mL | 0.9289 mL | 2.3223 mL | |
| 50 mM | 0.0743 mL | 0.3716 mL | 0.7431 mL | 1.8578 mL | |
| 60 mM | 0.0619 mL | 0.3096 mL | 0.6193 mL | 1.5482 mL |
Metoprine Related Classifications
HY-129441 Related Classifications
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