| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
EC50: 9.5 μM (PAD2); 0.4 μM (H3 citrullination)[1]
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|---|---|
| ln Vitro |
Compound 30a, or AFM-30a hydrochloride, exhibits an EC50 of 9.5 μM and high efficacy to penetrate HEK293T/PAD2 cells and covalently alter PAD2[1]. With an EC50 of 0.4 μM, AFM-30a hydrochloride exhibits good capacity to block H3 citrullination[1].
|
| ln Vivo |
In PAD2-/-transgenic mice, AFM-30a hydrochloride reduces airway remodeling and inhibits NLRP3 signaling[2].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HEK293T/PAD2 cells Tested Concentrations: Various concentrations Incubation Duration: 24 h Experimental Results: demonstrated low cytotoxicity for cells. |
| References |
[1]. Aaron Muth, et al. Development of a Selective Inhibitor of Protein Arginine Deiminase 2. J Med Chem. 2017 Apr 13;60(7):3198-3211.
[2]. R. Surolia, et al. Role of PAD2 Regulated Inflammasome Signaling in Arsenic Induced Airway Inflammation and Remodeling. American Journal of Respiratory and Critical Care Medicine 2020;201:A2976. |
| Molecular Formula |
C24H28CLFN6O3
|
|---|---|
| Molecular Weight |
502.97
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| Related CAS # |
AFM-30a;2095107-57-4
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| Solubility (In Vitro) |
H2O :~50 mg/mL (~99.41 mM)
DMSO :~50 mg/mL (~99.41 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (9.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9882 mL | 9.9410 mL | 19.8819 mL | |
| 5 mM | 0.3976 mL | 1.9882 mL | 3.9764 mL | |
| 10 mM | 0.1988 mL | 0.9941 mL | 1.9882 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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