Home Immunology & Inflammation SPHK activator Defensamide (MHP)

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Defensamide (MHP) SPHK activator

Cat.No.S6512

Defensamide (MHP) is an activator of sphingosine kinase (SPHK1) that modulates the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production.
Defensamide (MHP) SPHK activator Chemical Structure

Chemical Structure

Molecular Weight: 293.36

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S651201 DMSO]100 mg/mL]false]Water]100 mg/mL]false]Ethanol]Insoluble]false Purity: 99.78%
99.78

Chemical Information, Storage & Stability

Molecular Weight 293.36 Formula
C16H23NO4
 
 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1104874-94-3 -- Storage of Stock Solutions

Synonyms N/A Smiles CCCCCC(=O)NC(CC1=CC=C(C=C1)O)C(=O)OC

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (340.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.

Mechanism of Action

Targets/IC50/Ki
SPHK1 [1]
In vitro

Treatment with Defensamide (MHP) directly activates SPHK1 and increases cellular S1P content in normal cultured human keratinocytes. It also stimulates CAMP production and enhances epidermal antimicrobial defense via the recently identified S1P-dependent mechanism[1]. This compound also activates NF-κB which is assessed by nuclear translocation of NF-κB[2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04364230 Active not recruiting
Melanoma|Ocular Melanoma|Uveal Melanoma
Craig L Slingluff Jr|Celldex Therapeutics|University of Virginia
 September 28 2020 Phase 1|Phase 2
NCT02515227 Completed
Melanoma
Craig L Slingluff Jr|National Cancer Institute (NCI)|University of Virginia
 October 6 2016 Phase 1|Phase 2

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