VX-702

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的第二代 p38 MAPK 抑制剂，对 p38α 的 IC50 为 4-20 nM。

A potent, selective, second generation p38 MAPK inhibitor with IC50 of 4-20 nM for p38α; displays 14-fold higher potency against the p38α versus p38β; inhibits p38 activation induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen, without effect on collagen-mediated platelet aggregation.Rheumatoid Arthritis Phase 2 Discontinued(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 Cmax 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.

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VX702 | VX 702

MAPK/ERK Signaling

p38 MAPK

p38α

Inflammation/Immunology

Rheumatoid Arthritis

745833-23-2

404.3178

C19H12F4N4O2

>98% (HPLC)

DMSO: ≥ 42 mg/mL

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

3-Pyridinecarboxamide, 6-[(aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-

(-20℃)

With Ice Pack

≥ 2 years