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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
Molecular Weight:
436.26
MDL Number:
MFCD09834070
MOL File:
209410-46-8.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59

VX-745 Properties

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
FDA UNII TYL52QM320

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H332-H335
Precautionary statements  P261-P280-P305+P351+P338
HS Code  2933599590

VX-745 price More Price(37)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1638 VX-745 ≥98% (HPLC) 209410-46-8 5MG $108 2024-03-01 Buy
Sigma-Aldrich SML1638 VX-745 ≥98% (HPLC) 209410-46-8 25MG $435 2024-03-01 Buy
Cayman Chemical 18075 VX-745 ≥98% 209410-46-8 1mg $32 2024-03-01 Buy
Cayman Chemical 18075 VX-745 ≥98% 209410-46-8 5mg $139 2024-03-01 Buy
Cayman Chemical 18075 VX-745 ≥98% 209410-46-8 10mg $199 2024-03-01 Buy
Product number Packaging Price Buy
SML1638 5MG $108 Buy
SML1638 25MG $435 Buy
18075 1mg $32 Buy
18075 5mg $139 Buy
18075 10mg $199 Buy

VX-745 Chemical Properties,Uses,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.

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

Global( 141)Suppliers
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Capot Chemical Co.,Ltd.
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InvivoChem
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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-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 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 NEFLAMAPIMOD;VX 745 Neflamapimod (VX745, VRT031745 VD31745 Neflamapimod VX-745 MAPK inhibitor Inhibitor,VX745,Neflamapimod,Autophagy,VX 745,inhibit,p38 MAPK 209410-46-8 C19H9Cl2F2N3OS MAPK Aromatics Heterocycles Inhibitors Intermediates & Fine Chemicals Pharmaceuticals Sulfur & Selenium Compounds