1H-pyrazole
Based on 1 Customer Validation
1H-pyrazole (Pyrazole) is a five-membered heterocyclic compound, and its derivatives are orally effective antimalarial and antileishmanial agents with the potential to modulate targets such as alcohol dehydrogenase and NMDA receptors. 1H-pyrazole derivatives exhibit inhibitory effects on Plasmodium berghei in infected mice and on promastigotes of Leishmania aethiopica, respectively. 1H-pyrazole can be used in research related to malaria and leishmaniasis.
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- Pureza: 98.0%
- No. CAS: 288-13-1
- Fòrmula: C3H4N2
- Peso molecular:68.08
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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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
1H-pyrazole derivatives (0.04-10 μg/mL; 24 or 48 h) potently inhibit the growth of promastigotes of Leishmania aethiopica, with an IC50 of 0.079 μg/mL for compound 2; whereas other 1H-pyrazole derivatives (compound 3-9) exhibit varying degrees of anti-leishmanial activity, with IC50 values ranging from 0.2465 to 11.76 μg/mL[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:Swiss albino (male, 20-25 gm, malaria model via intravenous infection with Plasmodium berghei ANKA strain)[1]
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Dosage:48.4 μmol/kg
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Administration:p.o.; once daily; days 0-3
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Result:Achieved 70.26% parasitaemia suppression and mean survival time of 11 days (compound 3). Resulted in -55.9% parasitaemia suppression and mean survival time of 7.5 days (compound 2). Achieved 33.6% parasitaemia suppression and mean survival time of 9.1 days (compound 4). Achieved 27.9% parasitaemia suppression and mean survival time of 8.7 days (compound 5). Resulted in -15.1% parasitaemia suppression and mean survival time of 8.0 days (compound 6). Achieved 62.3% parasitaemia suppression and mean survival time of 9.4 days (compound 7). Resulted in -25.35% parasitaemia suppression and mean survival time of 7.8 days (compound 8). Resulted in -43.12% parasitaemia suppression and mean survival time of 7.4 days (compound 9).
Chemical Information
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No. CAS 288-13-1
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Appearance Solid
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Peso molecular 68.08
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Fòrmula C3H4N2
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Color Off-white to light brown
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SMILES
N1=CC=CN1
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Synonyms
Pyrazole
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Structure Classification
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Initial Source
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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
DMSO : 100 mg/mL (1468.86 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)
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 (36.72 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 (36.72 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.
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 (277 KB)
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SDS (806 KB)
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- Swedish - SV (806 KB)
- Italian - IT (806 KB)
- Korean - KR (806 KB)
- Portuguese - PT (806 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 14.6886 mL | 73.4430 mL | 146.8860 mL | 367.2150 mL |
| 5 mM | 2.9377 mL | 14.6886 mL | 29.3772 mL | 73.4430 mL | |
| 10 mM | 1.4689 mL | 7.3443 mL | 14.6886 mL | 36.7215 mL | |
| 15 mM | 0.9792 mL | 4.8962 mL | 9.7924 mL | 24.4810 mL | |
| 20 mM | 0.7344 mL | 3.6722 mL | 7.3443 mL | 18.3608 mL | |
| 25 mM | 0.5875 mL | 2.9377 mL | 5.8754 mL | 14.6886 mL | |
| 30 mM | 0.4896 mL | 2.4481 mL | 4.8962 mL | 12.2405 mL | |
| 40 mM | 0.3672 mL | 1.8361 mL | 3.6722 mL | 9.1804 mL | |
| 50 mM | 0.2938 mL | 1.4689 mL | 2.9377 mL | 7.3443 mL | |
| 60 mM | 0.2448 mL | 1.2241 mL | 2.4481 mL | 6.1203 mL | |
| 80 mM | 0.1836 mL | 0.9180 mL | 1.8361 mL | 4.5902 mL | |
| 100 mM | 0.1469 mL | 0.7344 mL | 1.4689 mL | 3.6722 mL |
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