1. MAPK/ERK Pathway Autophagy
  2. p38 MAPK Autophagy
  3. Neflamapimod

Neflamapimod  (Synonyms: VX-745)

目录号: HY-10328 纯度: 99.32%
COA 产品使用指南

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 p38αIC50 值为 10 nM,p38βIC50 值为 220 nM。Neflamapimod (VX-745) 具有抗炎活性。

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Neflamapimod Chemical Structure

Neflamapimod Chemical Structure

CAS No. : 209410-46-8

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10 mM * 1 mL in DMSO ¥600
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5 mg ¥550
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10 mg ¥880
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50 mg ¥3300
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查看 p38 MAPK 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 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) 表现出 PBMC IL-1β 和 TNFα IC50 值分别为 45 nM 和 51 nM。Neflamapimod 在全血中也有效,可阻断 IL-1β 和 TNFα 的释放,IC50 值分别为 150 nM 和 180 nM[1]
一种很有前途的选择性特征,p38α 的选择性是 p38β 的 20 倍 (Ki=220 nM)[1]
Neflamapimod (VX-745) 溶液在 DMSO/DMEM 中抑制 IL-6 的产生,IC50 为 15±9 nM[2]
Neflamapimod (VX-745;5.0 nM) 显示与密切相关的激酶 (包括 ERK1、JNK1-3 和 MK2) 相比,具有有效的活性和 1000 倍的选择性。Neflamapimod (10 nM-50 μM) 逐渐抑制茴香霉素诱导的 p38α 活性[3]
Neflamapimod (VX-745;0.06 μM -20 μM) 抑制 IL-6VEGF BMSC 中的分泌。Neflamapimod 可以抑制 BM 微环境中细胞因子 (TNF-α、IL-6、VEGF) 诱导的旁分泌 MM 细胞生长、存活和耐药性。Neflamapimod 以剂量依赖性方式诱导 MM.1S、RPMI8226 和 U266 细胞系的适度生长抑制,50% (IC50) 的抑制浓度为 10 μM[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Neflamapimod (VX-745;2.5、5 和 10 mg/kg) 可将小鼠的炎症评分分别提高 27%、31% 和 44%[1]。Neflamapimod (VX-745;1.06 mg/kg) 显著降低炎症评分,从对照组的 2.07±0.29 降至 1.42±0.06[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

436.26

Formula

C19H9Cl2F2N3OS

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 13.08 mg/mL (29.98 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2922 mL 11.4611 mL 22.9221 mL
5 mM 0.4584 mL 2.2922 mL 4.5844 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.32%

参考文献
Kinase Assay
[1]

Neflamapimod inhibits p38α and p38β. The IC50 for the inhibition of these two p38 homologs are obtained by a spectrophotometric coupled-enzyme assay. A fixed concentration of enzyme (15 nM of p38α or p38β) is incubated with various concentrations of Neflamapimod in DMSO for 10 min. at 30°C in 0.1 M HEPES buffer, pH 7.5, containing 10% glycerol, 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase, and 200 μM EGF receptor peptide. The reaction is initiated with 100 μM and 70 μM ATP for p38α and p38β assays, respectively. The decrease of absorbance at 340 nm is monitored to follow the rate of the reaction. IC50 is evaluated from the rate data as a function of the inhibitor concentration.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

For these experiments, cells are plated at a density of 60,000 cells/well in 96-well plates. Each condition is tested in triplicate or more. The following day, all particle suspensions, active substances or control solutions are freshly prepared, distributed and incubated for 24 h at 37°C. Then, supernatants are carefully discarded. To perform the MTT test, 50 μL of 0.1% MTT solution is added to each well for 3 h. Each well is then incubated for 1 h with 200 μL of dimethyl sulfoxide. Absorbance is measured at 595 nm. Reported results are expressed as the means±SD.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Type II collagen-induced arthritis is established in male DBA/1 mice with a minor modification. 10-Week old male DBA/1 mice are immunized by two intradermal injections within a 3 week interval using 100 μL of an emulsion consisting of a 1:1 (v/v) mixture of chick type II collagen (200 μg in 10 mM acetic acid) and complete Freund's adjuvant. Following the booster immunization, the mice are left untreated for 2-3 weeks, and are randomized into five treatment groups after they exhibit focal carpal (wrist) swelling (level 2 arthritic severity score) in both front paws. The five treatment groups are: 1: water control, 10 mL/kg, p.o., bid, (n=14); 2: 100% propylene glycol (PG) vehicle control, 10 mL/kg, p.o., bid, (n=8); 3: Neflamapimod in PG, at 10 mg/kg, p.o., bid, (n=7); 4: Neflamapimod in PG, at 5 mg/kg, p.o., bid, (n=10); and 5: Neflamapimod in PG, at 2.5 mg/kg, p.o., bid, (n=11). Arthritic symptoms are scored every other day using a level 1 to level 5 scoring system. Paw inflammation begins with erythema at the wrist (level 1), progressing to focal swelling of the wrist (level 2), to complete swelling of the wrist (level 3), to complete swelling of wrist and palm (level 4), and finally to complete swelling of wrist, palm and fingers (level 5). The sums of the scores from both front paw scores are used for plotting disease progression curves. Mice are sacrificed on day 20 and paws are removed, sectioned sagitally, stained with hemotoxylin & eosin, and scored for inflammation. Histologically, wrist joint inflammation begins with an infiltration of the synovium into the joint space (level 1), progressing to joint cartilage erosion (level 2), to joint cartilage and bone erosion (level 3), and finally to erosion of cartilage and bone accompanied by pannus formation (level 4).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Neflamapimod 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2922 mL 11.4611 mL 22.9221 mL 57.3053 mL
5 mM 0.4584 mL 2.2922 mL 4.5844 mL 11.4611 mL
10 mM 0.2292 mL 1.1461 mL 2.2922 mL 5.7305 mL
15 mM 0.1528 mL 0.7641 mL 1.5281 mL 3.8204 mL
20 mM 0.1146 mL 0.5731 mL 1.1461 mL 2.8653 mL
25 mM 0.0917 mL 0.4584 mL 0.9169 mL 2.2922 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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