| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
SR-318 targets p38 mitogen-activated protein kinase (MAPK), a family of serine/threonine kinases that play critical roles in cellular responses to stress, inflammation, and apoptosis. The compound shows high selectivity for p38α (IC₅₀ = 5 nM) and p38β (IC₅₀ = 32 nM). p38 MAPK is involved in the production of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6. By inhibiting p38 MAPK, SR-318 potently inhibits TNF-α release in whole blood with an IC₅₀ of 283 nM. The compound's anticancer activity is attributed to its ability to modulate cell signaling pathways involved in proliferation, survival, and apoptosis.
|
|---|---|
| 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].
In vitro, SR-318 is a potent and highly selective p38 MAPK inhibitor with IC₅₀ values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α/β. The compound potently inhibits TNF-α release in whole blood with an IC₅₀ of 283 nM. It exhibits anticancer and anti-inflammatory activities. The compound's high selectivity for p38α and p38β over other kinases makes it a valuable tool for studying p38 MAPK biology and for developing therapies for inflammatory diseases and cancer. Its in vitro activity is concentration-dependent, with efficacy observed at nanomolar to micromolar concentrations depending on the assay and target. |
| ln Vivo |
In vivo, SR-318 has potential applications in inflammatory diseases and cancer based on its p38 MAPK inhibitory activity. The compound's ability to potently inhibit TNF-α release in whole blood with an IC₅₀ of 283 nM suggests that it would be effective in animal models of inflammation. p38 MAPK inhibitors have been studied in various preclinical models for their anti-inflammatory and anti-cancer activities. However, detailed in vivo efficacy, pharmacokinetic, and toxicological data for SR-318 require further investigation from primary research publications. The compound is supplied as a research chemical for preclinical studies.
|
| Enzyme Assay |
In vitro enzyme/receptor binding (non-cellular) assays for SR-318 involve measuring inhibition of p38 MAPK kinase activity using purified recombinant enzymes. Kinase assays typically use a radioactive (³³P-ATP) or fluorescence-based method to detect phosphorylation of a peptide substrate (e.g., ATF-2 or MBP). The enzyme is incubated with varying concentrations of the compound, ATP, and substrate in kinase assay buffer (typically 50 mM HEPES, pH 7.5, with 10 mM MgCl₂ and 1 mM DTT). The reaction is terminated, and phosphorylated substrate is quantified. IC₅₀ values are calculated from concentration-response curves. The compound shows IC₅₀ values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α/β. Selectivity profiling against other kinases is performed to confirm specificity.
|
| Cell Assay |
In vitro cellular experiments with SR-318 are performed using various cell lines or whole blood to assess its anti-inflammatory and anticancer activities. For TNF-α release inhibition, whole blood is treated with LPS to stimulate TNF-α production and varying concentrations of SR-318. TNF-α levels in the supernatant are measured by ELISA. The compound shows an IC₅₀ of 283 nM. For anticancer studies, cancer cell lines are cultured in appropriate media and treated with varying concentrations of SR-318 for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. p38 MAPK signaling is assessed by measuring phosphorylation of downstream targets using Western blot analysis. Cells are maintained at 37°C in 5% CO₂ with appropriate media supplements.
|
| Animal Protocol |
In vivo animal studies with SR-318 have not been extensively reported. As a p38 MAPK inhibitor with anti-inflammatory and anticancer activities, standard in vivo models include rodent models of inflammation (e.g., LPS-induced endotoxemia, collagen-induced arthritis) and cancer (e.g., xenograft models). Animals are typically treated with SR-318 via oral, intraperitoneal, or intravenous administration at various doses. Efficacy is assessed by measuring inflammatory markers (TNF-α, IL-6), clinical scores, tumor volume, and survival. Pharmacodynamic markers such as p38 MAPK phosphorylation in target tissues may be measured to confirm target engagement. The compound shows potent inhibition of TNF-α release in whole blood, supporting its potential for in vivo efficacy.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of SR-318 are not extensively characterized. The compound has molecular formula C₂₇H₃₃N₅O₂ and molecular weight 459.58 g/mol. As a small molecule (molecular weight 459.58), it is expected to have reasonable oral bioavailability and cellular permeability. Storage: follow manufacturer's guidelines. Detailed pharmacokinetic parameters including half-life, clearance, and bioavailability require further investigation from primary research publications. The compound is supplied as a research chemical for preclinical studies.
|
| Toxicity/Toxicokinetics |
Toxicological information for SR-318 is not extensively detailed in the available literature. As a research compound with p38 MAPK inhibitory activity, it should be handled with appropriate safety precautions. Standard safety guidelines for handling potent pharmaceutical compounds apply, including use of personal protective equipment (gloves, safety goggles, lab coat) and working in a well-ventilated area. The compound is intended for research use only and is not approved for human therapeutic use. Cytotoxicity studies in cell-based assays help establish the therapeutic window and selectivity index of the compound.
|
| References | |
| Additional Infomation |
p38 MAP kinase inhibitors
SR-318 (CAS 2413286-32-3) is a potent and highly selective p38 MAPK inhibitor. The compound has molecular formula C₂₇H₃₃N₅O₂ and molecular weight 459.58 g/mol. SR-318 shows IC₅₀ values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α/β. The compound potently inhibits TNF-α release in whole blood with an IC₅₀ of 283 nM. SR-318 exhibits anticancer and anti-inflammatory activities. It is also known as SR 318. The compound is for research use only. |
| 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
|
| SMILES |
C1CCC(CC1)CCCNC(=O)C2=CC=C(C=C2)CNC(=O)C3=C(N(N=C3)C4=CC=CC=C4)N
|
| 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)
|
| 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. View More
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. |
| 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 |
*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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
