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

Name: Losmapimod
Brand: MedChemExpress
SKU: HY-10402
Rating: 5.0 (14 reviews)

Cat. No.: HY-10402 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

Losmapimod Chemical Structure

CAS No. : 585543-15-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 105	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 105	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 61	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
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

12 Publications Citing Use of MCE Losmapimod

: 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.

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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 pK_is 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.

585543-15-3

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
10 mM	0.2608 mL	1.3039 mL	2.6078 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

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 5

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)

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%

Select Batch:

Data Sheet (275 KB) SDS (418 KB)

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

Handling Instructions (2659 KB)

References

[1]. Willette RN, et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. J Pharmacol Exp Ther. 2009 Sep;330(3):964-70. [Content Brief]

[2]. Zhang XM, et al. Suppression of mitochondrial fission in experimental cerebral ischemia: The potential neuroprotective target of p38 MAPK inhibition. Neurochem Int. 2015 Nov;90:1-8. [Content Brief]

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

[1]. Willette RN, et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. J Pharmacol Exp Ther. 2009 Sep;330(3):964-70. [Content Brief]

[2]. Zhang XM, et al. Suppression of mitochondrial fission in experimental cerebral ischemia: The potential neuroprotective target of p38 MAPK inhibition. Neurochem Int. 2015 Nov;90:1-8. [Content Brief]

Complete Stock Solution Preparation Table

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

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

Customer Review

Losmapimod Related Antibodies

12 Publications Citing Use of MCE Losmapimod

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All p38 MAPK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Losmapimod Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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