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

Losmapimod (Synonyms: GSK-AHAB; GW856553X; SB856553)

Cat. No.: HY-10402 Purity: 97.08%
Handling Instructions

Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively.

For research use only. We do not sell to patients.
Losmapimod Chemical Structure

Losmapimod Chemical Structure

CAS No. : 585543-15-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 108 In-stock
10 mg USD 98 In-stock
50 mg USD 396 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    Losmapimod purchased from MCE. Usage Cited in: Neurochem Int. 2015 Nov;90:1-8.

    Inhibition of p38 MAPK (p38 inhibitor, Losmapimod 1 mg/kg) suppressed DLP1 and MFF with the temporal-accumulated effect after ischemia-reperfusion.

    Losmapimod purchased from MCE. Usage Cited in: EBioMedicine. 2018 Feb 1. pii: S2352-3964(18)30021-5.

    Western blot analysis of p-YAP, p-MKK3/6 and p-p38 expressions in untreated gefitinib-resistant cells (left, HCC827GR and right, H1975) or cells treated for 2, 6 or 10 h with Gefitinib (1 μM) or Losmapimod (1 μM) either alone or in combination. Total YAP, MKK3/6 and p38 MAPK proteins are used as loading controls.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively.

    IC50 & Target

    pKi: 8.1 (p38α), 7.6 (p38β)

    In Vivo

    In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β)[1].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.6078 mL 13.0392 mL 26.0783 mL
    5 mM 0.5216 mL 2.6078 mL 5.2157 mL
    10 mM 0.2608 mL 1.3039 mL 2.6078 mL
    Please refer to the solubility information to select the appropriate solvent.
    Animal Administration
    [1]

    Male SHR-SPs (n=70) are randomly assigned according to body weight into five groups (n=14 per group): normal diet controls (ND), high salt-fat diet controls (SFD), SFD + GSK-AHAB (1.2 mg/kg/day), and SFD + GSK-AHAB (12 mg/kg/day) and SFD + rofecoxib (18 mg/kg/day). All drugs are administered in the diet by mixing with the SFD. A subgroup of animals from each group (n=6 per group) are anesthetized with isoflurane and surgically instrumented with radiotelemetry units for the conscious measurement of mean arterial blood pressure and heart rate. These animals are allowed to recover for at least 7 days before the start of the study. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    383.46

    Formula

    C₂₂H₂₆FN₃O₂

    CAS No.

    585543-15-3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 58 mg/mL

    Losmapimod is prepared in PBS[2].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Product Name:
    Losmapimod
    Cat. No.:
    HY-10402
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