- VX-702
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- $45.00
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2026-06-02
- CAS:745833-23-2
- Purity: 99.19%
- Supply Ability: 10g
- VX 702
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- $100.00
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2023-08-16
- CAS:745833-23-2
- Min. Order: 1KG
- Purity: 99.9%
- Supply Ability: 50000kg/Month
- VX 702
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- $7.00
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2019-07-06
- CAS: 745833-23-2
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 100KG
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| | VX 702 Chemical Properties |
| Boiling point | 555.2±60.0 °C(Predicted) | | density | 1.503 | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 2 mg/ml) | | form | solid | | pka | 10.65±0.50(Predicted) | | color | White | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | | InChI | 1S/C19H12F4N4O2/c20-9-4-5-10(14(23)8-9)16-11(18(24)28)6-7-15(26-16)27(19(25)29)17-12(21)2-1-3-13(17)22/h1-8H,(H2,24,28)(H2,25,29) | | InChIKey | FYSRKRZDBHOFAY-UHFFFAOYSA-N | | SMILES | Fc1c(c(ccc1)F)N(c2nc(c(cc2)C(=O)N)c3c(cc(cc3)F)F)C(=O)N | | CAS DataBase Reference | 745833-23-2 |
| WGK Germany | WGK 3 | | HS Code | 2933399990 | | Storage Class | 11 - Combustible Solids |
| | VX 702 Usage And Synthesis |
| Biological activity | VX-702 is a highly selective p38α MAPK inhibitor, 14-fold more potent against p38α than against p38β. Phase 2. | | Description | VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion. It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively. VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 , or collagen but does not block platelet aggregation in response to collagen. Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis. | | Uses | VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion. It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively. VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 , or collagen but does not block platelet aggregation in response to collagen. Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.[Cayman Chemical] | | Uses | VX-702 is a p38 mitogen-activated protein kinase (MAPK) inhibitor. VX-702 had no effect on platelet aggregation induced by any of the p38 MAPK agonists. VX-702 has potential use in the treatment of inflammation, rheumatoid arthritis and cardiovascular diseases. | | Definition | ChEBI: 6-(N-carbamoyl-2,6-difluoroanilino)-2-(2,4-difluorophenyl)-3-pyridinecarboxamide is a phenylpyridine. | | 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]. | | storage | +4°C | | References | [1] DAVID M. GOLDSTEIN*. Selective p38α Inhibitors Clinically Evaluated for the Treatment of Chronic Inflammatory Disorders[J]. Journal of Medicinal Chemistry, 2009, 53 6: 2345-2353. DOI:10.1021/jm9012906
[2] ATHAN KULIOPULOS Lidija C Ramon Mohanlal. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation.[J]. Thrombosis and haemostasis, 2004, 92 6: 1387-1393. DOI:10.1160/th04-03-0187
[3] NEMANJA DAMJANOV George T S G Robert S Kauffman. Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: Results of two randomized, double-blind, placebo-controlled clinical studies?[J]. Arthritis & Rheumatology, 2009, 60 5: 1232-1241. DOI:10.1002/art.24485
[4] DING C. Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome.[J]. Current opinion in investigational drugs, 2006, 7 11: 1020-1025.
[5] ANDREY SKRIPCHENKO. An inhibition of p38 mitogen activated protein kinase delays the platelet storage lesion.[J]. PLoS ONE, 2013: e70732. DOI:10.1371/journal.pone.0070732 |
| | VX 702 Preparation Products And Raw materials |
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