Biological activity
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VX 702

Biological activity
Product Name
VX 702
CAS No.
745833-23-2
Chemical Name
VX 702
Synonyms
VX 702;CS-1840;VX702;VX-702;VX-702 ,S6005;VX 702 USP/EP/BP;(479543-46-9) vx 702;VX-702, 10 mM in DMSO;VX-702,VX702,VX 702,Inhibitor,p38 MAPK,inhibit,Autophagy;2-(2,4-Difluorophenyl)-6-(1-(2,6-difluorophenyl)ureido)nicotinamide;6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide
CBNumber
CB02484952
Molecular Formula
C19H12F4N4O2
Formula Weight
404.32
MOL File
745833-23-2.mol
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VX 702 Property

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)
pka
10.65±0.50(Predicted)
form 
solid
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.
CAS DataBase Reference
745833-23-2
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Safety

HS Code 
2933399990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2493
Product name
VX-702
Purity
≥98% (HPLC)
Packaging
5 mg
Price
$84.66
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2493
Product name
VX-702
Purity
≥98% (HPLC)
Packaging
25 mg
Price
$314
Updated
2025/07/31
TCI Chemical
Product number
V0147
Product name
VX-702
Purity
>98.0%(HPLC)
Packaging
25mg
Price
$147
Updated
2025/07/31
TCI Chemical
Product number
V0147
Product name
VX-702
Purity
>98.0%(HPLC)
Packaging
100mg
Price
$439
Updated
2025/07/31
Cayman Chemical
Product number
13108
Product name
VX-702
Purity
≥95%
Packaging
5mg
Price
$25
Updated
2024/03/01
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VX 702 Chemical Properties,Usage,Production

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 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.

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]

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

Raw materials

Preparation Products

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VX 702 Suppliers

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15402
Advantage
60
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
Advantage
62
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
SYN|thesis med chem P/L
Tel
+86-021-50720296
Fax
+86-021-50720297
Email
service@synkinase.com
Country
China
ProdList
266
Advantage
58
TOKYO CHEMICAL INDUSTRY CO., LTD.
Tel
03-36680489
Fax
03-3668-0520
Email
Sales-JP@TCIchemicals.com
Country
Japan
ProdList
28387
Advantage
80
CEG Chemical Science&Technology Co., Ltd.
Tel
Mobile:13665161512
Fax
+86-510-68873513
Country
China
ProdList
1785
Advantage
58
Shanghai HuanChuan Industry Co.,Ltd.
Tel
021-61478794
Fax
021-61478794
Email
sales@hcshhai.com
Country
China
ProdList
9793
Advantage
50
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View Lastest Price from VX 702 manufacturers

Weijer International Trade (Hebei) Co., Ltd
Product
VX 702 745833-23-2
Price
US $100.00/KG
Min. Order
1KG
Purity
99.9%
Supply Ability
50000kg/Month
Release date
2023-03-17
Career Henan Chemical Co
Product
VX 702 745833-23-2
Price
US $7.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2018-08-20

745833-23-2, VX 702Related Search:


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  • VX-702, 10 mM in DMSO
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