ChemicalBook > CAS DataBase List > VX-745

VX-745

Product Name
VX-745
CAS No.
209410-46-8
Chemical Name
VX-745
Synonyms
CS-1918;VD31745;VX-745, >=96%;VX-745(VX 745);VX-745 (Free base);NEFLAMAPIMOD;VX 745;Naluzotan Hydrochloride;Neflamapimod, 10 mM in DMSO;Neflamapimod (VX745, VRT031745;VX-745, p38 alpha MAPK inhibitor
CBNumber
CB8511364
Molecular Formula
C19H9Cl2F2N3OS
Formula Weight
436.26
MOL File
209410-46-8.mol
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VX-745 Property

Melting point:
261-264 °C
Boiling point:
578.9±60.0 °C(Predicted)
Density 
1.55±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
≥21.8 mg/mL in DMSO; insoluble in H2O; ≥2.1 mg/mL in EtOH with gentle warming and ultrasonic
form 
powder
pka
-0.97±0.40(Predicted)
color 
white to beige
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Safety

HS Code 
2933599590
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H332Harmful if inhaled

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1638
Product name
VX-745
Purity
≥98% (HPLC)
Packaging
5MG
Price
$108
Updated
2024/03/01
Sigma-Aldrich
Product number
SML1638
Product name
VX-745
Purity
≥98% (HPLC)
Packaging
25MG
Price
$435
Updated
2024/03/01
Cayman Chemical
Product number
18075
Product name
VX-745
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
18075
Product name
VX-745
Purity
≥98%
Packaging
5mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
18075
Product name
VX-745
Purity
≥98%
Packaging
10mg
Price
$199
Updated
2024/03/01
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VX-745 Chemical Properties,Usage,Production

Description

VX-745 is an inhibitor of p38α MAPK (IC50 = 9 nM). It is selective for p38α over p38β MAPK (Ki = 220 nM) as well as ERK, JNK, and a panel of 50 kinases when used at a concentration of 2 μM. VX-745 inhibits LPS-induced production of IL-1β and TNF-α in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 45 and 51 nM, respectively). It reduces disease severity in a type II collagen-induced mouse model of arthritis when administered at a dose of 10 mg/kg.

Chemical Properties

Pale Yellow Solid

Uses

VX 745 is a potent and selective inhibitor of p38α mitogen-activated protein (MAP) kinase. VX 745 is a potential anti-inflammatory agents. Studies suggest that VX 745 may be useful in the treatment of Werner syndrome.

Definition

ChEBI: A member of the class of pyrimidopyridazines that is 6H-pyrimido[1,6-b]pyridazin-6-one substituted at positions 2 and 5 by (2,4-difluorophenyl)sulfanyl and 2,6-dichlorophenyl groups respectively

Biochem/physiol Actions

VX-745 is a selective blood-brain barrier penetrant inhibitor of p38 MAPKα. VX-745 showed 20-fold selectivity for p38α over p38β and a Ki value of 220 nM. VX-745 has been shown to reduce inflammation in an arthritic (AIA) mouse model and to improve performance in aged rats.

storage

-20°C

References

[1]. bagley, m.c., et al., microwave-assisted ullmann c-s bond formation: synthesis of the p38alpha mapk clinical candidate vx-745. j org chem, 2009. 74(21): p. 8336-42.
[2]. dent, p., et al., mapk pathways in radiation responses. oncogene, 2003. 22(37): p. 5885-96.
[3]. dominguez, c., d.a. powers, and n. tamayo, p38 map kinase inhibitors: many are made, but few are chosen. curr opin drug discov devel, 2005. 8(4): p. 421-30.
[4]. duffy, j.p., et al., the discovery of vx-745: a novel and selective p38alpha kinase inhibitor. acs med chem lett, 2011. 2(10): p. 758-63.
[5]. bagley, m.c., et al., gram-scale synthesis of the p38alpha mapk-inhibitor vx-745 for preclinical studies into werner syndrome. future med chem, 2010. 2(9): p. 1417-27.

VX-745 Preparation Products And Raw materials

Raw materials

Preparation Products

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VX-745 Suppliers

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209410-46-8, VX-745Related Search:

Sulfadiazine Dichlorodiphenylsilane Dichloromethylphenylsilane Dichloroethane Sodium dichloroisocyanurate Triphenylphosphine Thionyl chloride Quinclorac Telaprevir Tozasertib Lumacaftor (VX-809) VX 702 Tofacitinib citrate Enzalutamide Quizartinib (AC220) SGX-523 1H-Pyrrole-2-carboxaMide, 4-[2-[(2-chloro-4-fluorophenyl)aMino]-5-Methyl-4-pyriMidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]- Pictilisib

  • 6H-PYRIMIDO[1,6-B]PYRIDAZIN-6-ONE, 5-(2,6-DICHLOROPHENYL)-2-[(2,4-DIFLUOROPHENYL)THIO]- (9CI)
  • 6H-PYRIMIDO[1,6-B]PYRIDAZIN-6-ONE, 5-(2,6-DICHLOROPHENYL)-2-[(2,4-DIFLUOROPHENYL)THIO]-
  • 5-(2,6-Dichlorophenyl)-2-((2,4-difluorophenyl)thio)-6H-pyrimido[1,6-b]pyridazin-6-on
  • 5-(2,6-Dichlorophenyl)-2-((2,4-difluorophenyl)thio)-6H-pyrimido[1,6-B]pyridazine-6-one
  • CS-1918
  • 5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenylthio)-6H-pyrimido[1,6-b]pyridazin-6-one
  • 5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenyl)sulfanylpyridazino[6,1-f]pyrimidin-6-one
  • 5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenylsulfanyl)-6H-pyriMido[3,4-b]pyridazin-6-one
  • VX-745(VX 745)
  • 5-(2,6-Dichloro-phenyl)-2-(2,4-difluoro-phenylsulfanyl)-1,7,8a-triaza-naphthalen-6-one
  • 5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenyl)sulfanylpyridazino[6,1-f]pyrimidin-6-one VX-745
  • VX-745 5-(2,6-Dichlorophenyl)-2-((2,4-difluorophenyl)thio)-6H-pyrimido[1,6-b]pyridazin-6-one
  • VX-745, >=96%
  • VX-745 (Free base)
  • Naluzotan Hydrochloride
  • NEFLAMAPIMOD;VX 745
  • Neflamapimod (VX745, VRT031745
  • VD31745
  • Neflamapimod VX-745 MAPK inhibitor
  • Inhibitor,VX745,Neflamapimod,Autophagy,VX 745,inhibit,p38 MAPK
  • 5-(2,6-dichlorophenyl)-2-[(2,4-difluorophenyl)sulfanyl]-6H-pyrimido[1,6-b]pyridazin-6-one
  • VX-745, p38 alpha MAPK inhibitor
  • Neflamapimod, 10 mM in DMSO
  • 209410-46-8
  • C19H9Cl2F2N3OS
  • MAPK
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Sulfur & Selenium Compounds