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 (VX745, VRT031745;Neflamapimod VX-745 MAPK inhibitor;Inhibitor,VX745,Neflamapimod,Autophagy,VX 745,inhibit,p38 MAPK
- CBNumber
- CB8511364
- Molecular Formula
- C19H9Cl2F2N3OS
- Formula Weight
- 436.26
- MOL File
- 209410-46-8.mol
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
Safety
- HS Code
- 2933599590
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.
N-Bromosuccinimide Price
- Product number
- SML1638
- Product name
- VX-745
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $108
- Updated
- 2024/03/01
- Product number
- SML1638
- Product name
- VX-745
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $435
- Updated
- 2024/03/01
- Product number
- 18075
- Product name
- VX-745
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 18075
- Product name
- VX-745
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 18075
- Product name
- VX-745
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $199
- Updated
- 2024/03/01
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
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