Losmapimod (GW856553X)

Name: Losmapimod (GW856553X)
Brand: Selleck Chemicals
SKU: S7215
Rating: 5 (11 reviews)

For research use only.

Catalog No.S7215 Synonyms: GW856553, GSK-AHAB

11 publications

Losmapimod (GW856553X) Chemical Structure

CAS No. 585543-15-3

Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pK_i of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.

Selleck's Losmapimod (GW856553X) has been cited by 11 publications

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

Free Radic Biol Med, 2021, 167:243-257

PubMed: 33746041 ( click the link to review the publication )

Mol Cell, 2020, 80(6):1104-1122.e9

PubMed: 33259812 ( click the link to review the publication )

Nat Microbiol, 2020, 10.1038/s41564-020-0782-1

PubMed: 32895527 ( click the link to review the publication )

Front Immunol, 2020, 11:363

PubMed: 32184787 ( click the link to review the publication )

J Pharmacol Exp Ther, 2020, 374(3):489-498

PubMed: 32576599 ( click the link to review the publication )

Cell Signal, 2020, 68:109528

PubMed: 31917191 ( click the link to review the publication )

J Neurogenet, 2018, 32(2):106-117

PubMed: 29718742 ( click the link to review the publication )

Pharmacol Res, 2018, 128:244-251

PubMed: 29079427 ( click the link to review the publication )

Oncotarget, 2018, 9(51):29680-29697

PubMed: 30038713 ( click the link to review the publication )

Auton Autacoid Pharmacol, 2015, 35(3):32-40

PubMed: 26913580 ( click the link to review the publication )

1 Customer Review

Intracellular pathways of b-adrenoceptor-induced proliferation. Urothelial proliferation (% of basal responses) in T24 in the absence and presence of (d) losmapimod (1-30 μM).

Auton Autacoid Pharmacol, 2015, 35(3):32-40.. Losmapimod (GW856553X) purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Biological Activity

Description

Targets

p38α ^[1] (Cell-free assay)	p38β ^[1] (Cell-free assay)
8.1(pKi)	7.6(pKi)

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
PBMC	NW\CW\|ByTnWwY4Tpc44h[XO\|YYm=		M4LUc\|EhcA>?		MYLJcohq[mm2aX;uJI9nKHB\|OHHsdIhiNWSncHXu[IVvfCCWTl\hcJBp[SCycn;keYN1cW:wIHnuJIh2dWGwIGDCUWMheHKnaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCOUGOgZ4hidGynbnflJIJ6KEWOSWPBMEBKSzVyPUCuNUDPxE1?	NXPISWd5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3O\|IzQDdpPkG5O\|czOjh5PD;hQi=>

... Click to View More Cell Line Experimental Data

In vivo

In spontaneously hypertensive stroke-prone rats (SHR-SP), Losmapimod significantly improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and subsequently attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1beta (IL-1beta). ^[1]

Protocol

Animal Research: ^[1]	- Collapse Animal Models: Spontaneously hypertensive stroke-prone rats Dosages: ~12 mg/kg Administration: p.o. (Only for Reference)

References

[1] Willette RN, et al. J Pharmacol Exp Ther. 2009, 330(3), 964-970.

Solubility (25°C)

In vitro	DMSO	76 mg/mL (198.19 mM)
	Water	Insoluble
	Ethanol	'41 mg/mL warmed

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Losmapimod (GW856553X) SDF

Molecular Weight	383.46
Formula	C₂₂ H₂₆ F N₃ O₂
CAS No.	585543-15-3
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	GW856553, GSK-AHAB
Smiles	CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04264442	Enrolling by invitation	Drug: Losmapimod	Facioscapulohumeral Muscular Dystrophy (FSHD)	Fulcrum Therapeutics	February 13 2020	Phase 2
NCT04004000	Active not recruiting	Drug: Losmapimod	Facioscapulohumeral Muscular Dystrophy 1	Fulcrum Therapeutics	August 23 2019	Phase 2
NCT02000440	Completed	Drug: Losmapimod	Glomerulosclerosis Focal Segmental	GlaxoSmithKline	July 1 2014	Phase 2
NCT00976560	Completed	Drug: GW856553\|Other: Placebo	Depressive Disorder Major	GlaxoSmithKline	September 25 2009	Phase 2
NCT00969059	Completed	Drug: GW856553\|Drug: PLACEBO	Pain Neuropathic	GlaxoSmithKline	August 2009	Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

p38 MAPK Signaling Pathway Map

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Losmapimod (GW856553X)