VX-745

Bezeichnung:VX-745

CAS-Nr209410-46-8

Englisch Name:VX-745

CBNumberCB8511364

SummenformelC19H9Cl2F2N3OS

Molgewicht436.26

MOL-Datei209410-46-8.mol

VX-745 physikalisch-chemischer Eigenschaften

Schmelzpunkt	261-264 °C
Siedepunkt	578.9±60.0 °C(Predicted)
Dichte	1.55±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	≥21.8 mg/mL in DMSO; insoluble in H2O; ≥2.1 mg/mL in EtOH with gentle warming and ultrasonic
Aggregatzustand	powder
pka	-0.97±0.40(Predicted)
Farbe	white to beige

Sicherheit

HS Code

2933599590

Gefahreninformationscode (GHS)

VX-745 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
VX-745 is an inhibitor of p38α MAPK (IC₅₀ = 9 nM). It is selective for p38α over p38β MAPK (K_i = 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.
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
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.
Lager
-20°C
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

209410-46-8, VX-745 Verwandte Suche:

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