Antibodies
VX-702
- 貨號 Cat. No.
- S6005
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
VX-702
VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2. | |||||
|---|---|---|---|---|---|---|
| Targets | p38 MAPKα | |||||
| IC50 | 4 - 20 nM [1] | |||||
| 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. [1] 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. [2] | |||||
| 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. [2]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. [3] 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.[4] | |||||
| Features | Highly selective, orally active inhibitor of p38 MAPK. | |||||
Protocol(Only for Reference)
Animal Study: [3]
| Animal Models | Mouse with collagen-induced arthritis |
|---|---|
| Dosages | ≤10 mg/kg |
| Administration | Administered via p.o. |
| Solubility | 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00205478 | Completed | Rheumatoid Arthritis | Vertex Pharmaceuticals Incorporated | 2005-06 | Phase 2 |
| NCT00395577 | Completed | Rheumatoid Arthritis | Vertex Pharmaceuticals Incorporated | 2006-11 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 404.3 |
|---|---|
| Formula | C19H12F4N4O2 |
| CAS No. | 745833-23-2 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 81 mg/mL (200 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.4043 | 4.043 | 8.086 | 12.129 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | Lee lay hoon from National University of Singapore. VX-702 purchased from Selleck | |
| Method | ELISA | |
| Cell Lines | Bone marrow derived macrophages | |
| Concentrations | 1-50 μM | |
| Incubation Time | 24 h | |
| Results | VX-702 treatment resulted in a reduction of TNF-a production. |
Product Citations (1)
