Home Metabolism Phospholipase (e.g. PLA) inhibitor Halobetasol Propionate

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Halobetasol Propionate Phospholipase (e.g. PLA) inhibitor

Cat.No.S4089

Halobetasol Propionate (BMY-30056, CGP-14458,Ulobetasol propionate) is an anti-inflammatory and a dermatologic agent commonly used to treat psoriasis.
Halobetasol Propionate Phospholipase (e.g. PLA) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 484.96

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Quality Control

Batch: S408901 DMSO]97 mg/mL]false]Ethanol]38 mg/mL]false]Water]Insoluble]false Purity: 99.92%
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99.92

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (200.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble

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In vivo
Batch:

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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.

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Chemical Information, Storage & Stability

Molecular Weight 484.96 Formula

C25H31ClF2O5

 Storage (From the date of receipt)
CAS No. 66852-54-8 Download SDF Storage of Stock Solutions

Synonyms BMY-30056, CGP-14458,Ulobetasol propionate Smiles CCC(=O)OC1(C(CC2C1(CC(C3(C2CC(C4=CC(=O)C=CC43C)F)F)O)C)C)C(=O)CCl

Mechanism of Action

Targets/IC50/Ki
PLA2
In vitro

Halobetasol propionate is thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. The initial interaction, however, is due to the drug binding to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes.
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03988439 Recruiting
Psoriasis
Bausch Health Americas Inc.
 March 24 2021 Phase 4
NCT03987763 Recruiting
Psoriasis
Bausch Health Americas Inc.
 October 22 2019 Phase 4

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