AR-C102222 hydrochloride
Based on 1 Customer Validation
AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM. AR-C102222 hydrochloride has antinociception and anti-inflammatory activities.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1781934-50-6
- Formula: C19H17ClF2N6O
- Molecular Weight:418.83
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
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Membrane Protein-targeted Compound Library
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Highly Selective Inhibitors Library
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Biological Activity
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iNOS |
AR-C102222 shows good efficacy in a rat adjuvant-induced arthritis model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Balb/c mice (20-25 g)[2].
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Dosage:3, 10, 30, 100 mg/kg.
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Administration:P.O. 55 min before the administration of 0.6% acetic acid (i.p., 1 mL/100 g volume).
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Result:Significantly inhibited arachidonic acid-induced ear inflammation following a dose of 100 mg/kg of has a maximal inhibition of approximately 79%.
Chemical Information
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CAS No. 1781934-50-6
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Appearance Solid
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Molecular Weight 418.83
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Formula C19H17ClF2N6O
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Color White to off-white
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SMILES
N#CC1=NC=C(C(N2CCC3(NC4=C(C(F)=CC=C4F)C(N)=N3)CC2)=O)C=C1.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (238.76 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 5 mg/mL (11.94 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 (11.94 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Tinker AC, et al. 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo. J Med Chem. 2003 Mar 13;46(6):913-6. [Content Brief]
[2]. LaBuda CJ, et al. Antinociceptive activity of the selective iNOS inhibitor AR-C102222 in rodent models of inflammatory, neuropathic and post-operative pain. Eur J Pain. 2006 Aug;10(6):505-12. Epub 2005 Aug 24. [Content Brief]
[3]. Yoon J, et al. Syntheses of 1,2,3-triazolyl salicylamides with inhibitory activity on lipopolysaccharide-induced nitric oxide production. Bioorg Med Chem Lett. 2011 Apr 1;21(7):1953-7. [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 (sealed storage, away from moisture). 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 | 2.3876 mL | 11.9380 mL | 23.8760 mL | 59.6901 mL |
| 5 mM | 0.4775 mL | 2.3876 mL | 4.7752 mL | 11.9380 mL | |
| 10 mM | 0.2388 mL | 1.1938 mL | 2.3876 mL | 5.9690 mL | |
| 15 mM | 0.1592 mL | 0.7959 mL | 1.5917 mL | 3.9793 mL | |
| 20 mM | 0.1194 mL | 0.5969 mL | 1.1938 mL | 2.9845 mL | |
| 25 mM | 0.0955 mL | 0.4775 mL | 0.9550 mL | 2.3876 mL | |
| 30 mM | 0.0796 mL | 0.3979 mL | 0.7959 mL | 1.9897 mL | |
| 40 mM | 0.0597 mL | 0.2985 mL | 0.5969 mL | 1.4923 mL | |
| 50 mM | 0.0478 mL | 0.2388 mL | 0.4775 mL | 1.1938 mL | |
| 60 mM | 0.0398 mL | 0.1990 mL | 0.3979 mL | 0.9948 mL | |
| 80 mM | 0.0298 mL | 0.1492 mL | 0.2985 mL | 0.7461 mL | |
| 100 mM | 0.0239 mL | 0.1194 mL | 0.2388 mL | 0.5969 mL |
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