2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Autophagy
  4. Losmapimod

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

Cat. No.: HY-10402 Purity: 99.96%
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Losmapimod (GSK-AHAB) est un inhibiteur de p38 MAPK qui est sélectif, puissant et oralement actif avec des pKis de 8,1 et 7,6 pour p38α et p38β, respectivement.

Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 105 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
1 mg USD 31 In-stock
5 mg USD 61 In-stock
10 mg USD 95 In-stock
50 mg USD 350 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 14 publication(s) in Google Scholar

Losmapimod Related Antibodies

Top Publications Citing Use of Products

    Losmapimod purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2018 Feb;28:51-61.  [Abstract]

    Western blot analysis of p-YAP, p-MKK3/6 and p-p38 expressions in untreated ZD1839-resistant cells (left, HCC827GR and right, H1975) or cells treated for 2, 6 or 10 h with ZD1839 (1 μM) or Losmapimod (1 μM) either alone or in combination. Total YAP, MKK3/6 and p38 MAPK proteins are used as loading controls.

    Losmapimod purchased from MedChemExpress. Usage Cited in: Neurochem Int. 2015 Nov;90:1-8.  [Abstract]

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

    View All p38 MAPK Isoform Specific Products:

    View All Isoforms
    p38 MAPK p38α p38β MAPK13 p38δ p38γ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively[1].

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    383.46

    Formula

    C22H26FN3O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1=C(C2=NC=C(C(NCC(C)(C)C)=O)C=C2)C=C(C(NC3CC3)=O)C=C1F
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    Ethanol : 33.33 mg/mL (86.92 mM; Need ultrasonic)

    DMSO : 27.5 mg/mL (71.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.75 mg/mL (7.17 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.75 mg/mL (7.17 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    COA (248 KB) HNMR (284 KB) LCMS (264 KB)

    Handling Instructions (2659 KB)
    References
    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 + MK 966 (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 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

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 2.6078 mL 13.0392 mL 26.0783 mL 65.1958 mL
    5 mM 0.5216 mL 2.6078 mL 5.2157 mL 13.0392 mL
    10 mM 0.2608 mL 1.3039 mL 2.6078 mL 6.5196 mL
    15 mM 0.1739 mL 0.8693 mL 1.7386 mL 4.3464 mL
    20 mM 0.1304 mL 0.6520 mL 1.3039 mL 3.2598 mL
    25 mM 0.1043 mL 0.5216 mL 1.0431 mL 2.6078 mL
    30 mM 0.0869 mL 0.4346 mL 0.8693 mL 2.1732 mL
    40 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6299 mL
    50 mM 0.0522 mL 0.2608 mL 0.5216 mL 1.3039 mL
    60 mM 0.0435 mL 0.2173 mL 0.4346 mL 1.0866 mL
    Ethanol 80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8149 mL
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    Losmapimod Related Classifications

    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.

    Keywords:

    Losmapimod585543-15-3GSK-AHAB GW856553X SB856553SB856553SB 856553SB-856553p38 MAPKAutophagyInhibitorinhibitorinhibit

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