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Chemical Structure| 585543-15-3 Chemical Structure| 585543-15-3

Structure of Losmapimod
CAS No.: 585543-15-3

Chemical Structure| 585543-15-3

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Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKi values of 8.1 for p38α and 7.6 for p38β.

Synonyms: GSK-AHAB; GW856553X; GW856553

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Product Details of Losmapimod

CAS No. :585543-15-3
Formula : C22H26FN3O2
M.W : 383.46
SMILES Code : O=C(NCC(C)(C)C)C1=CN=C(C2=CC(C(NC3CC3)=O)=CC(F)=C2C)C=C1
Synonyms :
GSK-AHAB; GW856553X; GW856553
MDL No. :MFCD16619322
InChI Key :KKYABQBFGDZVNQ-UHFFFAOYSA-N
Pubchem ID :11552706

Safety of Losmapimod

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

Related Pathways of Losmapimod

MAPK
TLR

Isoform Comparison

Biological Activity

Target
  • p38β

    p38β, pKi:7.6

  • p38α

    p38α, pKi:8.1

In Vitro:

Cell Line
Concentration Treated Time Description References
HCECs and RAW264.7 50 μg/mL 1 h To assess the anti-inflammatory effects of MTem/Los. PMC9189644
Human cardiac fibroblasts 30 µM 72 h Losmapimod reduces collagen expression in cultures infected with T. cruzi. PMC11242150
THP-1 cells 1 µM 1 h Assessment of cell proliferation and viability with treatment effects. PMC10407934

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice BAK-induced DED model Topical instillation 15.6 μg/kg twice per day for 14 days To evaluate the therapeutic effects of Losmapimod on DED. PMC9189644

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00517543 Chronic Obstructive Pulmonary ... More >>Disease (COPD)|Rheumatoid Arthritis|Atherosclerosis Less << PHASE1 COMPLETED 2025-10-07 GSK Investigational Site, Taco... More >>ma, Washington, 98418, United States Less <<
NCT00549653 Atherosclerosis|Cardiovascular... More >> Disease Less << PHASE1 COMPLETED 2025-12-07 GSK Investigational Site, Dall... More >>as, Texas, 75247, United States Less <<
NCT00474864 Healthy Subjects|Dyslipidaemia... More >>s|Dyslipidaemia Less << PHASE2 COMPLETED 2025-04-08 GSK Investigational Site, Camb... More >>ridge, CB2 2GG, United Kingdom|GSK Investigational Site, Cardiff, CF144XW, United Kingdom|GSK Investigational Site, London, EC1M 6BQ, United Kingdom Less <<
NCT04004000 Facioscapulohumeral Muscular D... More >>ystrophy 1 Less << PHASE2 TERMINATED 2024-10-31 Radboud University Medical Cen... More >>ter, Nijmegen, 9101, Netherlands Less <<
NCT02000440 Glomerulosclerosis, Focal Segm... More >>ental Less << PHASE2 COMPLETED 2016-05-11 GSK Investigational Site, Los ... More >>Angeles, California, 90025, United States|GSK Investigational Site, Stanford, California, 94304, United States|GSK Investigational Site, New Orleans, Louisiana, 70112, United States|GSK Investigational Site, Ann Arbor, Michigan, 48109, United States|GSK Investigational Site, Chapel Hill, North Carolina, 27599-7155, United States|GSK Investigational Site, Cleveland, Ohio, 44109, United States|GSK Investigational Site, Columbus, Ohio, 43210, United States|GSK Investigational Site, Philadelphia, Pennsylvania, 19140, United States|GSK Investigational Site, Edmonton, Alberta, T6G 2B7, Canada|GSK Investigational Site, Vancouver, British Columbia, V6Z 1Y6, Canada|GSK Investigational Site, Toronto, Ontario, M4N 3M5, Canada|GSK Investigational Site, Toronto, Ontario, M5G 2C4, Canada Less <<
NCT00599612 Pulmonary Disease, Chronic Obs... More >>tructive Less << PHASE1 COMPLETED 2008-02-18 GSK Investigational Site, Edin... More >>burgh, EH33 2NE, United Kingdom Less <<
NCT00256919 Arthritis, Rheumatoid PHASE2 COMPLETED 2025-11-06 GSK Investigational Site, Plov... More >>div, 4000, Bulgaria|GSK Investigational Site, Sofia, 1233, Bulgaria|GSK Investigational Site, Sofia, 1431, Bulgaria|GSK Investigational Site, Erlangen, Bayern, 91056, Germany|GSK Investigational Site, Muenchen, Bayern, 80639, Germany|GSK Investigational Site, Bad Bramstedt, Schleswig-Holstein, 24576, Germany|GSK Investigational Site, Hamburg, 21075, Germany|GSK Investigational Site, Madrid, 28046, Spain|GSK Investigational Site, Santiago de Compostela, 15706, Spain|GSK Investigational Site, Sevilla, 41071, Spain|GSK Investigational Site, Linkoeping, SE-582 25, Sweden|GSK Investigational Site, Uppsala, SE-753 23, Sweden|GSK Investigational Site, Donetsk, 83045, Ukraine|GSK Investigational Site, Kharkiv, 61002, Ukraine|GSK Investigational Site, Kiev, 01030, Ukraine|GSK Investigational Site, Kyiv, 03680, Ukraine|GSK Investigational Site, Lviv, 79010, Ukraine Less <<
NCT00392587 Pulmonary Disease, Chronic Obs... More >>tructive|Chronic Obstructive Pulmonary Disease (COPD) Less << PHASE2 COMPLETED - GSK Investigational Site, Hann... More >>over, Niedersachsen, 30625, Germany|GSK Investigational Site, Grosshansdorf, Schleswig-Holstein, 22927, Germany|GSK Investigational Site, Berlin, 14050, Germany Less <<
NCT00393146 Arthritis, Rheumatoid PHASE2 COMPLETED 2025-01-08 GSK Investigational Site, Buch... More >>arest, 11172, Romania|GSK Investigational Site, Bucharest, 20983, Romania|GSK Investigational Site, Moscow, 109240, Russian Federation|GSK Investigational Site, Moscow, 115093, Russian Federation|GSK Investigational Site, Moscow, 115522, Russian Federation|GSK Investigational Site, Moscow, 119049, Russian Federation|GSK Investigational Site, Moscow, 630117, Russian Federation|GSK Investigational Site, St Pertersburg, 196247, Russian Federation|GSK Investigational Site, Yaroslavl, 150003, Russian Federation|GSK Investigational Site, La Coru?a, 15006, Spain|GSK Investigational Site, Madrid, 28007, Spain|GSK Investigational Site, Madrid, 28034, Spain|GSK Investigational Site, Madrid, 28035, Spain|GSK Investigational Site, Madrid, 28046, Spain|GSK Investigational Site, Santiago de Compostela, 15706, Spain Less <<
NCT04264442 Facioscapulohumeral Muscular D... More >>ystrophy (FSHD) Less << PHASE2 TERMINATED 2024-11-07 University of California Irvin... More >>e, Irvine, California, 92868, United States|University of California Los Angeles (UCLA), Los Angeles, California, 90095, United States|University of Florida, Gainesville, Florida, 32610, United States|University of Kansas Medical Center, Kansas City, Kansas, 66160, United States|Kennedy Krieger Institute, Baltimore, Maryland, 21205, United States|University of Massachusetts Memorial Medical Center, Worcester, Massachusetts, 01655, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|University of Rochester Medical Center, Rochester, New York, 14642, United States|Ohio State University, Columbus, Ohio, 43221, United States|University of Utah, Salt Lake City, Utah, 84132, United States|Virginia Commonwealth University, Richmond, Virginia, 23298, United States|University of Washinton Medical Center, Seattle, Washington, 98195, United States|Ottawa Hospital Research Institute, Ottawa, Ontario, K1Y 4E9, Canada|Montreal Neurological Institute and Hospital, Montréal, Quebec, H3A 2B4, Canada|CHU de NICE- CHU pasteur2, Nice, 06001, France|Hospital de la Sta Creu i St Pau, Barcelona, 08041, Spain|Hospital UiP La Fe, Valencia, 46026, Spain Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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