R 29676
Based on 1 Customer Validation
R 29676 is a putative metabolite of Halopemide (HY-119093). R 29676 inhibits the binding of sodium-independent GABA to postsynaptic GABA receptors. R 29676 inhibits the binding of benzodiazepines to rat forebrain membranes. R 29676 inhibits sodium-dependent GABA binding to transporters and uptake, as well as Serotonin (HY-B1473A) uptake by rat platelets.
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- Purity : 99.80%
- CAS No.: 53786-28-0
- 화학식: C12H14ClN3O
- 분자량:251.72
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
79 μM
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Inhibition of serotonin uptake by rat blood platelets in a cell-based assay with an IC50 of 79 μM.
Inhibition of serotonin uptake by rat blood platelets in a cell-based assay with an IC50 of 79 μM.
|
2984638 |
In Vitro
R 29676 inhibits serotonin uptake by rat blood platelets with an IC50 of 79 μM[1].
R 29676 inhibits sodium-dependent GABA uptake by rat brain P2 homogenates with an IC50 of 280 μM[1].
R 29676 inhibits high-affinity sodium-independent [3H]GABA binding to rat brain membranes (GABA2 sites) with an IC50 of 11.6 μM[1].
R 29676 inhibits benzodiazepine binding to rat forebrain membranes with IC50 values of 127-160 μM[1].
R 29676 (300 µM; 5 min preincubation; 30 min incubation) inhibits sodium-dependent [3H]GABA binding to rat forebrain P2 membranes with an IC50 of 280 µM and produces 54% inhibition at 300 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 53786-28-0
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Appearance Solid
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분자량 251.72
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화학식 C12H14ClN3O
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Color White to off-white
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SMILES
C1=CC2=C(C=C1Cl)N=C(N2C3CCNCC3)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (397.27 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, 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: ≥ 5 mg/mL (19.86 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (19.86 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 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.
순도&문서
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Data Sheet (276 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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Handling Instructions (2659 KB)
References
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 | 3.9727 mL | 19.8633 mL | 39.7267 mL | 99.3167 mL |
| 5 mM | 0.7945 mL | 3.9727 mL | 7.9453 mL | 19.8633 mL | |
| 10 mM | 0.3973 mL | 1.9863 mL | 3.9727 mL | 9.9317 mL | |
| 15 mM | 0.2648 mL | 1.3242 mL | 2.6484 mL | 6.6211 mL | |
| 20 mM | 0.1986 mL | 0.9932 mL | 1.9863 mL | 4.9658 mL | |
| 25 mM | 0.1589 mL | 0.7945 mL | 1.5891 mL | 3.9727 mL | |
| 30 mM | 0.1324 mL | 0.6621 mL | 1.3242 mL | 3.3106 mL | |
| 40 mM | 0.0993 mL | 0.4966 mL | 0.9932 mL | 2.4829 mL | |
| 50 mM | 0.0795 mL | 0.3973 mL | 0.7945 mL | 1.9863 mL | |
| 60 mM | 0.0662 mL | 0.3311 mL | 0.6621 mL | 1.6553 mL | |
| 80 mM | 0.0497 mL | 0.2483 mL | 0.4966 mL | 1.2415 mL | |
| 100 mM | 0.0397 mL | 0.1986 mL | 0.3973 mL | 0.9932 mL |