A-943931
Based on 1 Customer Validation
A-943931 is a potent and selective histamine H4 receptor (H4R) antagonist with pKi values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.57%
- No. CAS: 1027330-97-7
- Fòrmula: C17H21N5
- Peso molecular:295.38
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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
- Pureza y Documentación
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Ver todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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Human H4 Receptor 4.6 nM (Ki) |
Rat H4 receptor 3.8 nM (Ki) |
A-943931 (10, 30, 100 µmol/kg; i.p.) shows antinociceptive efficacy in inflammatory pain and neuropathic pain model in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats (carrageenan-induced inflammatory pain and spinal nerve ligation model of neuropathic pain)[2]
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Dosage:10, 30, 100 µmol/kg
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Administration:I.p.
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Result:Showed antinociceptive efficacy in an inflammatory pain model in rat at an ED50 value of 72 µmol/kg, ip, and in a neuropathic pain model at an ED50 value of 100 µmol/kg, ip.
Chemical Information
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No. CAS 1027330-97-7
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Appearance Solid
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Peso molecular 295.38
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Fòrmula C17H21N5
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Color White to off-white
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SMILES
N[C@@H](C1)CCN1C2=C3CCCC4=CC=CC=C4C3=NC(N)=N2
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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 : 20 mg/mL (67.71 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)
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 mg/mL (6.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 3.3855 mL | 16.9273 mL | 33.8547 mL | 84.6367 mL |
| 5 mM | 0.6771 mL | 3.3855 mL | 6.7709 mL | 16.9273 mL | |
| 10 mM | 0.3385 mL | 1.6927 mL | 3.3855 mL | 8.4637 mL | |
| 15 mM | 0.2257 mL | 1.1285 mL | 2.2570 mL | 5.6424 mL | |
| 20 mM | 0.1693 mL | 0.8464 mL | 1.6927 mL | 4.2318 mL | |
| 25 mM | 0.1354 mL | 0.6771 mL | 1.3542 mL | 3.3855 mL | |
| 30 mM | 0.1128 mL | 0.5642 mL | 1.1285 mL | 2.8212 mL | |
| 40 mM | 0.0846 mL | 0.4232 mL | 0.8464 mL | 2.1159 mL | |
| 50 mM | 0.0677 mL | 0.3385 mL | 0.6771 mL | 1.6927 mL | |
| 60 mM | 0.0564 mL | 0.2821 mL | 0.5642 mL | 1.4106 mL |
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