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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
VX-702 is a novel, highly potent, orally bioavailable and selective inhibitor of p38α MAPK with potential anti-inflammatory activity. It has a 14-fold greater potency than p38β to inhibit p38α MAPK. It is one of the orally bioactive, second-generation p38 MAP kinase inhibitors that may be effective in the treatment of cardiovascular, inflammatory, and rheumatoid arthritis conditions. After exposure to 16 °C without agitation for 24 h, VX-702 prevents activation of p38MAPK and decreases in many platelet storage parameters.
| Targets |
p38α (IC50 = 4 nM-20 nM)
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| ln Vitro |
Pre-incubation of platelets with VX-702 (1 μM) prevents or reduces the activation of p38 (IC50 4 to 20 nM) brought on by platelet agonists like thrombin, SFLLRN, AYPGKF, U46619, and collagen. No matter whether anti-platelet medications are used or not, VX-702 has no impact on the platelet aggregation caused by any of the p38 MAPK agonists. [1] VX-702 dose-dependently reduces the production of IL-6, IL-1β and TNFα (IC50 = 59, 122, and 99 ng/mL, respectively). [2]
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| ln Vivo |
VX-702 has a volume of distribution of 73 L/kg, a half-life of 16 to 20 hours, and a median clearance of 3.75 L/h. For VX-702, which is primarily cleared renally, both AUC and Cmax values are dose proportional. [2] VX-702 has a similar impact to methotrexate (0.1 mg/kg) when administered twice daily at a dose of 0.1 mg/kg. By comparing the percentage inhibition of wrist joint erosion and inflammation score, VX-702 (5 mg/kg twice daily) also has an equivalent impact to prednisolone (10 mg/kg once daily). [3] VX-702 has no impact on ERKs or JNKs while selectively inhibiting the activation of p38 MAPK following ischemia. Compared to the 5 mg/kg and vehicle groups, the 50 mg/kg group's MI/AAR ratio is significantly lower. [4]
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| Enzyme Assay |
For the half-life Platelet activation caused by platelet agonists such as thrombin, SFLLRN, AYPGKF, U46619, and collagen is completely or partially inhibited (IC50 4 to 20 nM) by pre-incubating platelets with VX-702 (1 μM). In the presence or absence of anti-platelet therapies, VX-702 has no impact on the platelet aggregation brought on by any of the p38 MAPK agonists. IL-6, IL-1β and TNFα production are all inhibited by VX-702 in a dose-dependent manner (IC50 values are 59, 122, and 99 ng/mL, respectively).
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| Cell Assay |
VX-702 was administered in the isolated perfused rat kidney (IPRK) model at doses ranging from 100 to 600 ng/mL with linear excretion, and the clearance data were consistent with net reabsorption by the kidney. The renal organic anion and organic cation transport systems were also shown not to use VX-702 as a substrate.
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| Animal Protocol |
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| References |
| Molecular Formula |
C19H12F4N4O2
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| Molecular Weight |
404.3
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| Exact Mass |
404.09
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| Elemental Analysis |
C, 56.44; H, 2.99; F, 18.80; N, 13.86; O, 7.91
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| CAS # |
745833-23-2
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| 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
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| InChi Key |
FYSRKRZDBHOFAY-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
6-(N-carbamoyl-2,6-difluoroanilino)-2-(2,4-difluorophenyl)pyridine-3-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4734 mL | 12.3671 mL | 24.7341 mL | |
| 5 mM | 0.4947 mL | 2.4734 mL | 4.9468 mL | |
| 10 mM | 0.2473 mL | 1.2367 mL | 2.4734 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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