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 分子式: C₁₉H₁₂F₄N₄O₂ 分子量: 404.32 EC番号: 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

概要

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

同義語

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

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

作用メカニズム

MAP kinase p38 alpha inhibitor

名前と識別子

異性体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

代替CAS番号

479543-46-9

PubChem CID

10341154

分子量

404.32

関連ターゲット（人間）

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)

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro DMSO: 71 mg/mL (199.15 mM); Water: Insoluble; Ethanol: Insoluble
• 屈折率: n20D1.63 (Predicted)