Home GPCR & G Protein Endothelin Receptor antagonist Sparsentan (PS-433540, RE-021)

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Sparsentan (PS-433540, RE-021) Endothelin Receptor antagonist

Cat.No.S6665

Sparsentan (PS-433540, RE-021, DARA) is a dual endothelin type A receptor(ETA) and angiotensin II type 1 receptor antagonist.
Sparsentan (PS-433540, RE-021) Endothelin Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 592.75

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Quality Control

Batch: S666501 DMSO]100 mg/mL]false]Ethanol]40 mg/mL]false]Water]Insoluble]false Purity: 99.71%
99.71

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (168.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 40 mg/mL

Water : Insoluble

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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.

Chemical Information, Storage & Stability

Molecular Weight 592.75 Formula

C32H40N4O5S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 254740-64-2 -- Storage of Stock Solutions

Synonyms DARA Smiles CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC(=C(C=C3)C4=CC=CC=C4S(=O)(=O)NC5=NOC(=C5C)C)COCC

Mechanism of Action

Targets/IC50/Ki
endothelin type A receptor
angiotensin II type 1 receptor
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05572229 Not yet recruiting
Multiple Myeloma
University Hospital Lille|Janssen Pharmaceutica N.V. Belgium
 September 2023 Phase 2
NCT05408026 Withdrawn
Relapsed or Refractory Multiple Myeloma
Alliance Foundation Trials LLC.|Janssen LP|Celgene
 October 1 2022 Phase 1|Phase 2
NCT05004259 Active not recruiting
Hemolytic Anemia
Dartmouth-Hitchcock Medical Center
 March 21 2022 Phase 1

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