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

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

Cat. No.: HY-10402 Purity: 99.94%
COA
SDS
Handling Instructions Technical Support

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 585543-15-3

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

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

고객리뷰

Based on 12 publication(s) in Google Scholar

Other Forms of Losmapimod:

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 Akt1 p38α p38β MAPK13 p38δ p38γ

    • Biological Activity

    • Protocol

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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
    분자량

    383.46

    화학식

    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
    선적

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

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

    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.

    • 몰농도 계산기

    • 농도 희석 계산기

    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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.52 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% EtOH    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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.
    Calculation results:
    Working solution concentration: mg/mL
    순도&문서

    Purity: 99.94%

    SDS (418 KB)

    COA (248 KB) HNMR (285 KB) LCMS (94 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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    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
    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
    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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    상품명:
    Losmapimod
    Cat. No.:
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    SAFETY DATA SHEET (SDS)

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