SR-318 (SR318) is a novel and potent p38 MAPK inhibitor with anti-cancer and anti-inflammatory activity. It inhibits p38α and p38β with IC50s of 5 and 32 nM, respectively. SR 318 also inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 0.283 µM).
Physicochemical Properties
| Molecular Formula | C₂₇H₃₃N₅O₂ |
| Molecular Weight | 459.58 |
| Exact Mass | 459.263 |
| CAS # | 2413286-32-3 |
| PubChem CID | 139030333 |
| Appearance | White to off-white solid powder |
| Density | 1.24±0.1 g/cm3(Predicted) |
| Boiling Point | 732.0±60.0 °C(Predicted) |
| LogP | 5.6 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 9 |
| Heavy Atom Count | 34 |
| Complexity | 639 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | HXNUFFCHRIWTRZ-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C27H33N5O2/c28-25-24(19-31-32(25)23-11-5-2-6-12-23)27(34)30-18-21-13-15-22(16-14-21)26(33)29-17-7-10-20-8-3-1-4-9-20/h2,5-6,11-16,19-20H,1,3-4,7-10,17-18,28H2,(H,29,33)(H,30,34) |
| Chemical Name | 5-amino-N-[[4-(3-cyclohexylpropylcarbamoyl)phenyl]methyl]-1-phenylpyrazole-4-carboxamide |
| Synonyms | SR318 SR 318 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | As a pharmacologic probe, SR-318 is a strong and specific inhibitor of p38α/β type II that can be utilized to target this particular inactive state of both p38 isoforms [1]. |
| References |
[1]. Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors. J Med Chem. 2019 Dec 12;62(23):10757-10782. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~125 mg/mL (~271.99 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.53 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 20.8 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: ≥ 2.08 mg/mL (4.53 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 20.8 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (4.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1759 mL | 10.8795 mL | 21.7590 mL | |
| 5 mM | 0.4352 mL | 2.1759 mL | 4.3518 mL | |
| 10 mM | 0.2176 mL | 1.0879 mL | 2.1759 mL |