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Chemical Structure| 209410-46-8 Chemical Structure| 209410-46-8

Structure of Neflamapimod
CAS No.: 209410-46-8

Chemical Structure| 209410-46-8

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Neflamapimod (VX-745) is an effective, blood-brain barrier-penetrant, highly selective p38α inhibitor, with IC50 values of 10 nM for p38α and 220 nM for p38β. Neflamapimod (VX-745) exhibits anti-inflammatory activity.

Synonyms: VX-745

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Product Details of Neflamapimod

CAS No. :209410-46-8
Formula : C19H9Cl2F2N3OS
M.W : 436.26
SMILES Code : O=C1N=CN2N=C(SC3=CC=C(F)C=C3F)C=CC2=C1C4=C(Cl)C=CC=C4Cl
Synonyms :
VX-745
MDL No. :MFCD09834070
InChI Key :VEPKQEUBKLEPRA-UHFFFAOYSA-N
Pubchem ID :3038525

Safety of Neflamapimod

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Related Pathways of Neflamapimod

MAPK
TLR

Isoform Comparison

Biological Activity

Target
  • p38β

    p38β, IC50:220 nM

  • p38α

    p38α, IC50:10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
U251MG 50 μM 48 hours NEF inhibits TMZ-induced upregulation of PDIA3P1 PMC9284800
GSC267 50 μM 48 hours NEF inhibits TMZ-induced upregulation of PDIA3P1 PMC9284800
GSC20 50 μM 48 hours NEF inhibits TMZ-induced upregulation of PDIA3P1 PMC9284800
Rat mesenteric artery smooth muscle cells 0.0001–10 µM 2–3 minutes To investigate the acute inhibitory effect of Neflamapimod on mesenteric arteries, results showed that Neflamapimod produced concentration-dependent vasodilation PMC8941071
LN229 50 μM 48 hours NEF inhibits TMZ-induced upregulation of PDIA3P1 PMC9284800
U87MG 50 μM 48 hours NEF inhibits TMZ-induced upregulation of PDIA3P1 PMC9284800
U118MG 50 μM 48 hours NEF inhibits TMZ-induced upregulation of PDIA3P1 PMC9284800

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague Dawley rats Mesenteric artery model In vitro perfusion 10 µM Single administration, lasting 30 minutes To study the vasodilatory effect of Neflamapimod on mesenteric arteries, results showed that Neflamapimod induced vasodilation by inhibiting p38 MAPKα and its downstream Hsp27 phosphorylation PMC8941071
BALB/c nude mice Glioblastoma xenograft model Oral 5 mg/kg 5 times per week NEF combined with TMZ exhibited excellent synergistic anti-tumor effects in vivo PMC9284800

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04001517 Dementia With Lewy Bodies (DLB... More >>) Less << PHASE2 COMPLETED 2020-06-30 University of California San D... More >>iego (UCSD), La Jolla, California, 92037, United States|Pacific Neuroscience Institute, Santa Monica, California, 90404, United States|University of Colorado, Aurora, Colorado, 80045, United States|Elite Clinical Research, Miami, Florida, 33144, United States|University of Kansas Medical Center, Kansas City, Kansas, 66103, United States|Massachusetts General Hospital, Charlestown, Massachusetts, 02129, United States|University of Michigan, Ann Arbor, Michigan, 48105, United States|Mayo Clinic, Rochester, Minnesota, 55905, United States|Cleveland Clinic - Lou Ruvo Center for Brain Health, Las Vegas, Nevada, 89106, United States|New York Presbyterian Hospital - Columbia University Medical Center, New York, New York, 10032, United States|University of Rochester, Rochester, New York, 14618, United States|University of North Carolina, Chapel Hill, North Carolina, 27599, United States|Cleveland Clinic, Cleveland, Ohio, 44195, United States|The Ohio State University, Columbus, Ohio, 43210, United States|Summit Research Network, Portland, Oregon, 97210, United States|Oregon Health & Science University, Portland, Oregon, 97239, United States|Thomas Jefferson University, Philadelphia, Pennsylvania, 19107, United States|University of Virginia, Charlottesville, Virginia, 22908, United States|National Clinical Research, Inc., Richmond, Virginia, 23294, United States|Northwest Clinical Research Center, Bellevue, Washington, 98007, United States|University of Washington, Seattle, Washington, 98104, United States|Inland Northwest Research, Spokane, Washington, 99202, United States|Brain Research Center, Amsterdam, Netherlands|Brain Research Center, Den Bosch, Netherlands Less <<
NCT02423200 Alzheimer's Disease PHASE2 COMPLETED 2025-11-16 Parexel International, Glendal... More >>e, California, 91206, United States Less <<
NCT02423122 Alzheimer's Disease|Mild Cogni... More >>tive Impairment Less << PHASE2 COMPLETED 2025-09-16 Alzheimer Research Center, VU ... More >>Medical Center, Amsterdam, 1081 HV, Netherlands Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.46mL

2.29mL

1.15mL

22.92mL

4.58mL

2.29mL

References

 

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