Neflamapimod
Based on 12 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.32%
- CAS 番号: 209410-46-8
- 分子式: C19H9Cl2F2N3OS
- 分子量:436.26
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-10256
Adezmapimodp38 MAPK Inhibitor -
HY-10402
Losmapimodp38α/β MAPK Inhibitor -
HY-10320
Doramapimodp38 MAPK Inhibitor -
HY-10456
TAK-715p38 MAPK Inhibitor -
HY-16782
PexmetinibTie-2/p38 MAPK Inhibitor -
HY-13241
Ralimetinib dimesylateApoptosis Inducer -
HY-10578
PD 169316p38 MAP Kinase Inhibitor -
HY-10406
Talmapimodp38α MAPK Inhibitor -
HY-10401
VX-702p38α MAPK Inhibitor -
HY-11068
SB 239063p38 MAPK Inhibitor -
HY-10295
SB 202190p38 MAPK Inhibitor -
HY-10403
PH-797804p38α/β Inhibitor
MedChemExpress（MCE）の使用を引用している文献 Neflamapimod
More- Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Basic Res Cardiol. 2026 Oct;121(5):837-862.
- Biochem Pharmacol. 2023 Aug:214:115683. [Abstract]
- Colloids Surf B Biointerfaces. 2026 May 19:266:115827. [Abstract]
- bioRxiv. 2023 Jun 25.
- bioRxiv. 2023 Jan 17.
- Research Square Preprint. 2022 May.
- Research Square Preprint. 2022 May.
- Research Square Preprint. 2021 Dec.
- bioRxiv. 2020 Apr.
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Cell Proliferation/Viability Assay
-
ELISA
-
WB
-
IF
生物活性
製品説明
IC50 & Target
[5]|
p38α 10 nM (IC50) |
p38β 220 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
0.039 μM
Compound: VX-745
|
Inhibition of LPS-induced TNFalpha production in human THP1 cells
Inhibition of LPS-induced TNFalpha production in human THP1 cells
|
[PMID: 18325768] |
| THP-1 | IC50 |
150 nM
Compound: 3
|
Inhibition of LPS-induced p38-related Tumor necrosis factor alpha release by THP-1 cells
Inhibition of LPS-induced p38-related Tumor necrosis factor alpha release by THP-1 cells
|
[PMID: 12540232] |
| THP-1 | IC50 |
56 nM
Compound: VX-745
|
Inhibition of LPS-stimulated TNFalpha production in THP1 cells
Inhibition of LPS-stimulated TNFalpha production in THP1 cells
|
[PMID: 16750367] |
体外実験
Neflamapimod (VX-745) exhibits PBMC IL-1β and TNFα IC50 values of 45 and 51 nM, respectively. Neflamapimod is also effective in whole blood, blocking IL-1β and TNFα release with IC50 values 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 IC50 of 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 209410-46-8
-
性状 Solid
-
分子量 436.26
-
分子式 C19H9Cl2F2N3OS
-
Color Light yellow to yellow
-
SMILES
O=C1N=CN(C(C=C2)=C1C3=C(Cl)C=CC=C3Cl)N=C2SC4=CC=C(F)C=C4F
-
別名
VX-745
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (12)
-
Journal Impact Factor
-
Most Recent
-
Nat Nanotechnol
Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]2021 Jul;16(7):830-839. PMID: 33958764 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
-
Biochem Pharmacol
Neflamapimod inhibits endothelial cell activation, adhesion molecule expression, leukocyte attachment and vascular inflammation by inhibiting p38 MAPKα and NF-κB signaling. [Abstract]2023 Aug:214:115683. PMID: 37429422
Neflamapimod purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Aug:214:115683. [Abstract]
Neflamapimod (Nefla, 10-100 nM; 16 h) inhibited LPS-stimulated induction of ICAM-1 on MECs. Mean ELISA data showing induction of ICAM-1 by LPS (10 µg) and suppression of ICAM-1 expression by 10 and 100 nM Neflamapimod.
Neflamapimod purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Aug:214:115683. [Abstract]
Neflamapimod (Nefla, 10-100 nM; 16 h) inhibited LPS-stimulated induction of ICAM-1 on MECs. Representative Western blot images showing ICAM-1 induction by LPS and inhibition of ICAM-1 expression by 1, 10 and 100 nM Neflamapimod treatment in MECs.
Neflamapimod purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Aug:214:115683. [Abstract]
Neflamapimod (Nefla, 2.5-10 mg/kg; p.o.; twice daily for two days) treatment reduced LPS-mediated ICAM-1 induction in rat aortas in vivo.
Neflamapimod purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Aug:214:115683. [Abstract]
Neflamapimod (Nefla, 2.5-10 mg/kg; p.o.; twice daily for two days) treatment reduced LPS-mediated VCAM-1 induction in rat aortas in vivo.
-
Colloids Surf B Biointerfaces
Nanotechnology-based encapsulation of neflamapimod: A new therapeutic strategy for lewy body dementia. [Abstract]2026 May 19:266:115827. PMID: 42160963
Neflamapimod purchased from MedChemExpress. Usage Cited in: Colloids Surf B Biointerfaces. 2026 May 19:266:115827. [Abstract]
Cell viability of SH-SY5Y and U87-MG treated cells. Cells were exposed to INV-NEFLA (black), unloaded INV (red), or Neflamapimod (NEFLA) alone (green) at concentrations ranging from 1 to 1000 μg/ml lipids, and cell viability was assessed at 24 h using XTT assay.
Neflamapimod purchased from MedChemExpress. Usage Cited in: Colloids Surf B Biointerfaces. 2026 May 19:266:115827. [Abstract]
Cell viability of SH-SY5Y and U87-MG treated cells. Cells were exposed to INV-NEFLA (black), unloaded INV (red), or Neflamapimod (NEFLA) alone (green) at concentrations ranging from 1 to 1000 μg/ml lipids, and cell viability was assessed at 48 h using XTT assay.
-
-
-
-
-
-
溶剤 & 溶解度
体外:
DMSO : 12.5 mg/mL (28.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (11.46 mM); Suspended solution; Need ultrasonic
純度とドキュメンテーション
-
データシート (285 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Duffy JP, et al. The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor. ACS Med Chem Lett. 2011 Jul 28;2(10):758-63. [Content Brief]
[2]. Cicenas J, et al. JNK, p38, ERK, and SGK1 Inhibitors in Cancer. Cancers (Basel). 2017 Dec 21;10(1). [Content Brief]
[3]. Pradal J, et al. Intra-articular bioactivity of a p38 MAPK inhibitor and development of an extended-release system. Eur J Pharm Biopharm. 2015 Jun;93:110-7. [Content Brief]
[4]. Alam JJ. Selective Brain-Targeted Antagonism of p38 MAPKα Reduces Hippocampal IL-1β Levels and Improves Morris Water Maze Performance in Aged Rats. J Alzheimers Dis. 2015;48(1):219-27. [Content Brief]
[5]. Bagley MC, et al. Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5107-10. Epub 2007 Jul 13. [Content Brief]
[6]. Hideshima T, et al. Targeting p38 MAPK inhibits multiple myeloma cell growth in the bone marrow milieu. Blood, 2003, 101(2), 703-705. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |
Neflamapimod 関連分類
HY-10328 関連分類
Powered by Bioz