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Sparsentan

Catalog No. T5355 CAS 254740-64-2

Synonyms: DARA-a, RE-021

Sparsentan is a first-in-class orally active and highly potent dual endothelin A and angiotensin II receptor antagonist(Ki of 9.3 and 0.8 nM, respectively)

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Sparsentan, CAS 254740-64-2

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sparsentan is a first-in-class orally active and highly potent dual endothelin A and angiotensin II receptor antagonist(Ki of 9.3 and 0.8 nM, respectively)
Targets&IC50	Human endothelin A:9.3 nM(ki) , Human angiotensin II:0.8 nM(ki) , Rat angiotensin II:0.4 nM(ki)

Synonyms	DARA-a, RE-021
Molecular Weight	592.76
Formula	C32H40N4O5S
CAS No.	254740-64-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 240 mg/mL (404.89 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Murugesan N, et al. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9. 2. Komers R , Diva U , Inrig J K , et al. Study Design of the Phase 3 Sparsentan vs Irbesartan (DUPLEX) Study in Patients With Focal Segmental Glomerulosclerosis (FSGS)[J]. Kidney International Reports, 2020, 5(4). 3. Komers R , Gipson D S , Nelson P , et al. Efficacy and Safety of Sparsentan Compared With Irbesartan in Patients With Primary Focal Segmental Glomerulosclerosis: Randomized, Controlled Trial Design (DUET)[J]. Kidney International Reports, 2017:654-664.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Cardiovascular Disease Compound Library Endocrinology-Hormone Compound Library Inhibitor Library Drug Repurposing Compound Library Bioactive Compound Library Clinical Compound Library

Related Products

Related compounds with same targets

Camellianin A Ramiprilat [Sar1, Ile8]-Angiotensin II Azilsartan Methyl Ester Angiotensin II (3-8), human BIBS 39 Aliskiren D6 hemifumarate Pratosartan

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Sparsentan 254740-64-2 G蛋白偶联受体内分泌与激素 RAAS Endothelin Receptor RE 021 Inhibitor inhibit Angiotensin Receptor RE-021 RE021 DARA-a inhibitor

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