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Neflamapimod
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Neflamapimod图片
CAS NO:209410-46-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
VX-745
产品介绍
Neflamapimod (VX-745) 是有效的,可穿过血脑屏障的,高选择性的p38α抑制剂,对 p38α 的IC50值为 10 nM,p38β 的IC50值为 220 nM。Neflamapimod (VX-745) 具有抗炎活性。
生物活性

Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor ofp38αinhibitor with anIC50forp38αof 10 nM and forp38βof 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.

IC50& Target[5]

p38α

10 nM (IC50)

p38β

220 nM (IC50)

体外研究
(In Vitro)

Neflamapimod (VX-745) exhibits PBMC IL-1β and TNFα IC50values of 45 and 51 nM, respectively. Neflamapimod is also effective in whole blood, blocking IL-1β and TNFα release with IC50values of 150 and 180 nM, respectively[1].
Neflamapimod shows a promising selectivity profile, with 20-fold selectivity for p38α over p38β (Ki=220 nM)[1].
Neflamapimod (VX-745) solutions in DMSO/DMEM inhibits the IL-6 production with IC50of 15±9 nM[2].
Neflamapimod (VX-745; 5.0 nM) displays potent activity and 1000-fold selectivity over closely related kinases, including ERK1, JNK1-3 and MK2. Neflamapimod (10 nM-50 μM) increasingly inhibits the anisomycin-induced activity of p38α[3].
Neflamapimod (VX-745; 0.06 μM-20 μM) inhibits IL-6 and VEGF secretion in BMSCs. Neflamapimod can inhibit cytokine (TNF-α, IL-6, VEGF)-induced paracrine MM cell growth, survival, and drug resistance in the BM microenvironment. Neflamapimod induces modest growth inhibition of MM.1S, RPMI8226, and U266 cell lines in a dose-dependent fashion, with inhibitory concentration of 50% (IC50) of 10 μM[4].

体内研究
(In Vivo)

Neflamapimod (VX-745; 2.5, 5, and 10 mg/kg) improves the inflammatory scores in mice by 27%, 31%, and 44%, respectively[1]. Neflamapimod (VX-745; 1.06 mg/kg) significantly decreases the inflammation score from 2.07±0.29 for the control group to 1.42±0.06[2].

Clinical Trial
分子量

436.26

性状

Solid

Formula

C19H9Cl2F2N3OS

CAS 号

209410-46-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 13.08 mg/mL(29.98 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2922 mL11.4611 mL22.9221 mL
5 mM0.4584 mL2.2922 mL4.5844 mL
10 mM0.2292 mL1.1461 mL2.2922 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。