VX-702 - 10mM in DMSO , MAP kinase p38 alpha inhibitor, CAS No.745833-23-2, MAP kinase p38 alpha inhibitor

CAS: 745833-23-2 Cat. No.: V408898 Formule: C₁₉H₁₂F₄N₄O₂ Poids moléculaire: 404.32 Numéro CE: 833-998-9 PubChem CID: 10341154

GRADE & PURITY 10mM in DMSO

Synonyms

1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Vue d’ensemble

Information

VX-702 is a highly selective inhibitor ofp38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.
In vitro

Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner.

In vivo

The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and C_max values are dose proportional for VX-702, which is predominantly cleared renally. VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score. VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Synonymes

1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea

Spécifications et pureté

10mM in DMSO

Mécanismes biochimiques et physiologiques

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

Conditions de stockage de stockage

Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Mécanisme d'action

MAP kinase p38 alpha inhibitor

Noms et identifiants

Isomères SMILES

C1=CC(=C(C(=C1)F)N(C2=NC(=C(C=C2)C(=O)N)C3=C(C=C(C=C3)F)F)C(=O)N)F

CAS alternatif

479543-46-9

PubChem CID

10341154

Poids moléculaire

404.32

Cibles associées (humaines)

MAPKAPK2 Tchem MAP kinase-activated protein kinase 2 (0 Activities)

Discover Target: MAPKAPK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ALK Tclin ALK tyrosine kinase receptor (0 Activities)

Discover Target: ALK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK11 Tchem Mitogen-activated protein kinase 11 (0 Activities)

Discover Target: MAPK11

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK14 Tchem Mitogen-activated protein kinase 14 (0 Activities)

Discover Target: MAPK14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MYLK Tchem Myosin light chain kinase, smooth muscle (0 Activities)

Discover Target: MYLK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriétés chimiques et physiques

• Solubilité: Solubility (25°C) In vitro DMSO: 71 mg/mL (199.15 mM); Water: Insoluble; Ethanol: Insoluble
• Indice de réfraction: n20D1.63 (Predicted)