VX-745
| Code | Size | Price |
|---|
| AG-CR1-3754-M001 | 1 mg | £30.00 |
Quantity:
| AG-CR1-3754-M005 | 5 mg | £90.00 |
Quantity:
| AG-CR1-3754-M010 | 10 mg | £150.00 |
Quantity:
| AG-CR1-3754-M050 | 50 mg | £500.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
AMBIENT
Storage:
Short Term: +4°C Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenylthio)-6H-pyrimido[1,6-b]pyridazin-6-one; Neflamapimod; VX745
Appearance:
Off-white to yellowish solid.
CAS:
209410-46-8
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.
InChi:
InChI=1S/C19H9Cl2F2N3OS/c20-11-2-1-3-12(21)17(11)18-14-5-7-16(25-26(14)9-24-19(18)27)28-15-6-4-10(22)8-13(15)23/h1-9H
InChiKey:
VEPKQEUBKLEPRA-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 209410-46-8. Formula: C19H9Cl2F2N3OS. MW: 436.3. 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).
MDL:
MFCD09834070
Molecular Formula:
C19H9Cl2F2N3OS
Molecular Weight:
436.3
Package Type:
Plastic Vial
Product Description:
VX-745 is a potent inhibitor of p38alpha MAPK (IC50=10nM) with 20-fold selectivity over p38beta and 1000-fold selectivity over closely related kinases, ERK1, MK2 and JNK1-3. p38alpha 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-alpha, IL-1beta and IL-6. VX-745 is an anti-inflammatory agent that blocks IL-1beta and TNF-alpha 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).
Purity:
>95%
SMILES:
FC1=CC(F)=C(SC2=NN(C=N3)C(C=C2)=C(C4=C(Cl)C=CC=C4Cl)C3=O)C=C1
Solubility Chemicals:
Soluble in DMSO (25mg/ml) or DMF (30mg/ml). Insoluble in water.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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 p38alpha 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 P38alpha kinase inhibitor: J.P. Duffy, et al.; ACS Med. Chem. Lett. 2, 758 (2011) | Neflamapimod: Clinical Phase 2b-Ready Oral Small Molecule Inhibitor of p38alpha to Reverse Synaptic Dysfunction in Early Alzheimer's Disease: J. Alam, et al.; J. Prev. Alzheimers Dis. 4, 273 (2017)