5,7-Dichloropyrazolo[1,5-a]pyrimidine
Based on 1 Customer Validation
5,7-Dichloropyrazolo[1,5-a]pyrimidine is a PDE10A inhibitor with a Ki of 24 μM. 5,7-Dichloropyrazolo[1,5-a]pyrimidine serves as a key intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives (HIV-1 non-nucleoside reverse transcriptase inhibitors). 5,7-Dichloropyrazolo[1,5-a]pyrimidine can be used for the research of schizophrenia.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 57489-77-7
- Formula: C6H3Cl2N3
- Molecular Weight:188.01
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Storage:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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PDE10A 24 μM (Ki) |
5,7-Dichloropyrazolo[1,5-a]pyrimidine inhibits recombinant PDE10A with a Ki of 24 μM and an LBE of 0.44 in a cell-free IMAP binding assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 57489-77-7
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Appearance Solid
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Molecular Weight 188.01
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Formula C6H3Cl2N3
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Color Off-white to light yellow
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SMILES
ClC1=CC(Cl)=NC2=CC=NN21
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 200 mg/mL (1063.77 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, 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.
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: ≥ 5 mg/mL (26.59 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Raheem IT, et al. Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. Bioorg Med Chem Lett. 2016;26(1):126-132. [Content Brief]
[2]. Tian Y, et al. Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives. Bioorg Med Chem. 2014 Apr 1;22(7):2052-9. [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 | 5.3189 mL | 26.5943 mL | 53.1887 mL | 132.9717 mL |
| 5 mM | 1.0638 mL | 5.3189 mL | 10.6377 mL | 26.5943 mL | |
| 10 mM | 0.5319 mL | 2.6594 mL | 5.3189 mL | 13.2972 mL | |
| 15 mM | 0.3546 mL | 1.7730 mL | 3.5459 mL | 8.8648 mL | |
| 20 mM | 0.2659 mL | 1.3297 mL | 2.6594 mL | 6.6486 mL | |
| 25 mM | 0.2128 mL | 1.0638 mL | 2.1275 mL | 5.3189 mL | |
| 30 mM | 0.1773 mL | 0.8865 mL | 1.7730 mL | 4.4324 mL | |
| 40 mM | 0.1330 mL | 0.6649 mL | 1.3297 mL | 3.3243 mL | |
| 50 mM | 0.1064 mL | 0.5319 mL | 1.0638 mL | 2.6594 mL | |
| 60 mM | 0.0886 mL | 0.4432 mL | 0.8865 mL | 2.2162 mL | |
| 80 mM | 0.0665 mL | 0.3324 mL | 0.6649 mL | 1.6621 mL | |
| 100 mM | 0.0532 mL | 0.2659 mL | 0.5319 mL | 1.3297 mL |