Synonym
SR-318; SR318; SR 318;
IUPAC/Chemical Name
5-Amino-N-(4-((3-cyclohexylpropyl)carbamoyl)benzyl)-1-phenyl-1H-pyrazole-4-carboxamide
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)
SMILES Code
O=C(C1=C(N)N(C2=CC=CC=C2)N=C1)NCC3=CC=C(C(NCCCC4CCCCC4)=O)C=C3
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
SR-318 is a dual inhibitor of p38α and p38β MAPKs (IC50s = 5 and 32 nM, respectively). It is selective for p38α and p38β MAPKs over a panel of 468 kinases at 1 µM. SR-318 inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 0.283 µM).
In vitro activity:
SR-318 presents a potent and selective type-II inhibitor of p38α/β that can be used as a chemical probe for targeting this particular inactive state of these two p38 isoforms. SR-318 had excellent potency and selectivity for p38α/β, potently inhibiting the TNF-α release in whole blood.
Reference: J Med Chem. 2019 Dec 12;62(23):10757-10782. https://pubmed.ncbi.nlm.nih.gov/31702918/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
40.0 |
87.03 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
459.59
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Röhm S, Schröder M, Dwyer JE, Widdowson CS, Chaikuad A, Berger BT, Joerger AC, Krämer A, Harbig J, Dauch D, Kudolo M, Laufer S, Bagley MC, Knapp S. Selective targeting of the αC and DFG-out pocket in p38 MAPK. Eur J Med Chem. 2020 Dec 15;208:112721. doi: 10.1016/j.ejmech.2020.112721. Epub 2020 Aug 20. PMID: 33035818.
2. Röhm S, Berger BT, Schröder M, Chaikuad A, Winkel R, Hekking KFW, Benningshof JJC, Müller G, Tesch R, Kudolo M, Forster M, Laufer S, Knapp S. Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors. J Med Chem. 2019 Dec 12;62(23):10757-10782. doi: 10.1021/acs.jmedchem.9b01227. Epub 2019 Nov 26. PMID: 31702918.
In vitro protocol:
1. Röhm S, Schröder M, Dwyer JE, Widdowson CS, Chaikuad A, Berger BT, Joerger AC, Krämer A, Harbig J, Dauch D, Kudolo M, Laufer S, Bagley MC, Knapp S. Selective targeting of the αC and DFG-out pocket in p38 MAPK. Eur J Med Chem. 2020 Dec 15;208:112721. doi: 10.1016/j.ejmech.2020.112721. Epub 2020 Aug 20. PMID: 33035818.
2. Röhm S, Berger BT, Schröder M, Chaikuad A, Winkel R, Hekking KFW, Benningshof JJC, Müller G, Tesch R, Kudolo M, Forster M, Laufer S, Knapp S. Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors. J Med Chem. 2019 Dec 12;62(23):10757-10782. doi: 10.1021/acs.jmedchem.9b01227. Epub 2019 Nov 26. PMID: 31702918.
1: [Double-blind evaluation of SR-318, a sustained release preparation of diclofenac sodium, on rheumatoid arthritis]. Ryumachi. 1988 Jun;28(3):188-98. Japanese. PMID: 3238539.
2: Röhm S, Berger BT, Schröder M, Chaikuad A, Winkel R, Hekking KFW, Benningshof JJC, Müller G, Tesch R, Kudolo M, Forster M, Laufer S, Knapp S. Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors. J Med Chem. 2019 Dec 12;62(23):10757-10782. doi: 10.1021/acs.jmedchem.9b01227. Epub 2019 Nov 26. PMID: 31702918.
3: Röhm S, Schröder M, Dwyer JE, Widdowson CS, Chaikuad A, Berger BT, Joerger AC, Krämer A, Harbig J, Dauch D, Kudolo M, Laufer S, Bagley MC, Knapp S. Selective targeting of the αC and DFG-out pocket in p38 MAPK. Eur J Med Chem. 2020 Dec 15;208:112721. doi: 10.1016/j.ejmech.2020.112721. Epub 2020 Aug 20. PMID: 33035818.
4: Duarte-Restrepo E, Noguera-Oviedo K, Butryn D, Wallace JS, Aga DS, Jaramillo- Colorado BE. Spatial distribution of pesticides, organochlorine compounds, PBDEs, and metals in surface marine sediments from Cartagena Bay, Colombia. Environ Sci Pollut Res Int. 2021 Mar;28(12):14632-14653. doi: 10.1007/s11356-020-11504-6. Epub 2020 Nov 20. PMID: 33216302.
