SAR113945 monopotassium
SAR113945 monopotassium is a highly selective IKK-β inhibitor with an IC50 value of 0.4 nM. SAR113945 monopotassium blocks the canonical NFκB signaling pathway. SAR113945 monopotassium alleviates hyperalgesia to heat and mechanical stimuli, and exerts effects in a zymosan-induced knee joint inflammation model. SAR113945 monopotassium is applicable to research related to symptomatic knee osteoarthritis.
For research use only. We do not sell to patients.
- CAS No.: 899418-65-6
- Formula: C28H24KN7O3
- Molecular Weight:545.63
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
All Adenosine Receptor Isoforms
More
Biological Activity
|
IKK-β 0.4 nM (IC50) |
Adenosine A3 receptor 0.89 μM (IC50) |
SAR113945 monopotassium potently inhibits the native IKK complex purified from HeLa cell extracts, with an IC50 of 0.018 μM[1].
SAR113945 (10 μM) monopotassium exhibits high kinase specificity. In a kinome panel comprising 62 kinases, it only inhibits mixed lineage kinase 1 (MLK1) by 59% at a concentration of 10 μM[1].
SAR113945 (10 μM) monopotassium exhibits high receptor and enzyme specificity, acting solely as an antagonist of the adenosine A3 receptor, with an IC50 of 0.89 μM in a screening panel comprising 106 targets[1].
SAR113945 (Compound 1) monopotassium inhibits IKK-β with an IC50 of 0.4 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Lewis rats (male)[1]
-
Dosage:0.01 mg per joint; 0.1 mg per joint; 1 mg per joint; 10 mg per joint
-
Administration:intra-articular; single dose
-
Result:Produced a maximum pain reduction of 88% at the highest dose of 10 mg per joint.
Was well tolerated.
Chemical Information
-
CAS No. 899418-65-6
-
Molecular Weight 545.63
-
Formula C28H24KN7O3
-
SMILES
O=C(O[K])[C@H](CN(C1=CC=CC=C1)C2=NC=CC=C2)NC(C3=CC4=C(NC(C5=NC(NC)=NC=C5)=C4)C=C3)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : ≥ 100 mg/mL (183.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
[1]. Grothe K, et al. IκB kinase inhibition as a potential treatment of osteoarthritis - results of a clinical proof-of-concept study. Osteoarthritis Cartilage. 2017 Jan;25(1):46-52. [Content Brief]
[2]. Liu D, et al. Small molecule inhibitors of osteoarthritis: Current development and future perspective. Frontiers in physiology. 2023;14:1156913. [Content Brief]
[3]. Noha SM, et al. Discovery of a novel IKK-β inhibitor by ligand-based virtual screening techniques. Bioorganic & medicinal chemistry letters. 2011 Jan 01;21(1):577-83. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8327 mL | 9.1637 mL | 18.3274 mL | 45.8186 mL |
| 5 mM | 0.3665 mL | 1.8327 mL | 3.6655 mL | 9.1637 mL | |
| 10 mM | 0.1833 mL | 0.9164 mL | 1.8327 mL | 4.5819 mL | |
| 15 mM | 0.1222 mL | 0.6109 mL | 1.2218 mL | 3.0546 mL | |
| 20 mM | 0.0916 mL | 0.4582 mL | 0.9164 mL | 2.2909 mL | |
| 25 mM | 0.0733 mL | 0.3665 mL | 0.7331 mL | 1.8327 mL | |
| 30 mM | 0.0611 mL | 0.3055 mL | 0.6109 mL | 1.5273 mL | |
| 40 mM | 0.0458 mL | 0.2291 mL | 0.4582 mL | 1.1455 mL | |
| 50 mM | 0.0367 mL | 0.1833 mL | 0.3665 mL | 0.9164 mL | |
| 60 mM | 0.0305 mL | 0.1527 mL | 0.3055 mL | 0.7636 mL | |
| 80 mM | 0.0229 mL | 0.1145 mL | 0.2291 mL | 0.5727 mL | |
| 100 mM | 0.0183 mL | 0.0916 mL | 0.1833 mL | 0.4582 mL |
SAR113945 monopotassium Related Classifications
HY-111970B Related Classifications
Powered by Bioz