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AdipoGen Life Sciences
VX-745
30
CHF
CHF 30.00
In stock
AG-CR1-3754-M0011 mgCHF 30.00
AG-CR1-3754-M0055 mgCHF 90.00
AG-CR1-3754-M01010 mgCHF 150.00
AG-CR1-3754-M05050 mgCHF 525.00
| Product Details | |
|---|---|
| Synonyms | 5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenylthio)-6H-pyrimido[1,6-b]pyridazin-6-one; Neflamapimod; VX745 |
| Product Type | Chemical |
| Properties | |
| Formula |
C19H9Cl2F2N3OS |
| MW | 436.3 |
| CAS | 209410-46-8 |
| Purity Chemicals | ≥98% |
| Appearance | Off-white to yellowish solid. |
| Solubility | Soluble in DMSO (25mg/ml) or DMF (30mg/ml). Insoluble in water. |
| Identity | Determined by 1H-NMR |
| InChi Key | VEPKQEUBKLEPRA-UHFFFAOYSA-N |
| Smiles | FC1=CC(F)=C(SC2=NN(C=N3)C(C=C2)=C(C4=C(Cl)C=CC=C4Cl)C3=O)C=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- VX-745 is a potent inhibitor of p38α MAPK (IC50=10nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1, MK2 and JNK1-3. p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases and is widely expressed in endothelial, immune or inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β and IL-6.
- VX-745 is an anti-inflammatory agent that blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180nM, respectively. VX-745 showed anti-inflammatory efficacy in an animal model of rheumatoid arthritis and recently anti-neuroinflammatory potential in prevention of early-stage Alzheimers diseases (AD).
Product References
- VX-745. Vertex Pharmaceuticals: J.J. Haddad; Curr. Opin. Investig. Drugs 2, 1070 (2001)
- Targeting p38 MAPK inhibits multiple myeloma cell growth in the bone marrow milieu: T. Hideshima, et al.; Blood 101, 703 (2003)
- Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders: D.M. Golstein, et al.; J. Med. Chem. 53, 2345 (2010)
- The discovery of VX-745: A novel and selective P38α kinase inhibitor: J.P. Duffy, et al.; ACS Med. Chem. Lett. 2, 758 (2011)
- Neflamapimod: Clinical Phase 2b-Ready Oral Small Molecule Inhibitor of p38α to Reverse Synaptic Dysfunction in Early Alzheimer's Disease: J. Alam, et al.; J. Prev. Alzheimers Dis. 4, 273 (2017)
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