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CAS

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254740-64-2

Sparsentan (RE-021) is a dual endothelin type A receptor (ETA) and angiotensin II type 1 receptor antagonist, also known as PS-433540, DARA, and irbesartan-ETA antagonist. It is a selective dual-acting receptor antagonist with affinity for both endothelin (A type) and angiotensin II receptors (Type 1). Sparsentan combines the active moieties of the selective AT1 receptor antagonist irbesartan and a selective ETA receptor antagonist.

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  • 2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-(ethoxymethyl)phenyl]-N-(4,5-dimethyl-1,2-oxazol-3-yl)benzenesulfonamide

    Cas No: 254740-64-2

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  • 254740-64-2 Structure

  • Basic information

    1. Product Name: Sparsentan (RE-021)
    2. Synonyms: Sparsentan (RE-021);Sparsentan-d5 (RE-021-d5);RE 201;[1,1'-Biphenyl]-2-sulfonamide, 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-;Sparsentan;4'-[(2-Butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide;4'-((2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl)-N-(4,5-dimethylisoxazol-3-yl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide
    3. CAS NO:254740-64-2
    4. Molecular Formula: C32H40N4O5S
    5. Molecular Weight: 592.7488
    6. EINECS: N/A
    7. Product Categories: N/A
    8. Mol File: 254740-64-2.mol

  • Chemical Properties

    1. Melting Point: 148 °C(Solv: isopropanol (67-63-0); water (7732-18-5))
    2. Boiling Point: 744.4±70.0 °C(Predicted)
    3. Flash Point: N/A
    4. Appearance: /
    5. Density: 1.28±0.1 g/cm3(Predicted)
    6. Refractive Index: N/A
    7. Storage Temp.: N/A
    8. Solubility: N/A
    9. PKA: 7.06±0.50(Predicted)
    10. CAS DataBase Reference: Sparsentan (RE-021)(CAS DataBase Reference)
    11. NIST Chemistry Reference: Sparsentan (RE-021)(254740-64-2)
    12. EPA Substance Registry System: Sparsentan (RE-021)(254740-64-2)

  • Safety Data

    1. Hazard Codes: N/A
    2. Statements: N/A
    3. Safety Statements: N/A
    4. WGK Germany:
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 254740-64-2(Hazardous Substances Data)

254740-64-2 Usage

Uses

Used in Pharmaceutical Industry:
Sparsentan (RE-021) is used as an Endothelin A receptor antagonist for the treatment of hypertension. It helps regulate blood pressure by blocking the action of endothelin and angiotensin II, which are hormones that constrict blood vessels and increase blood pressure.
Additionally, Sparsentan (RE-021) has potential applications in the treatment of other conditions related to the constriction of blood vessels and high blood pressure, such as heart disease and kidney disease. Its dual-action mechanism makes it a promising candidate for the development of new therapies to manage these conditions more effectively.

Biological Activity

Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.

in vitro

Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED50 value of 0.8 μmol/kg iv and 3.6 μmol/kg po. Sparsentan also shows efficacious and long acting in the big ET-1-induced pressor model. Sparsentan causes a significant lowering of blood pressure at the lowest dose tested (10 μmol/kg/day) in spontaneously hypertensive rats. Sparsentan shows good oral bioavailability in rats, dogs, and monkeys, averaging 40%, 86%, and 21% F, respectively. At 100 μmol/kg/day, Sparsentan reduces the blood pressure from 170 to less than 100 mmHg during the course of the drug’s pharmacokinetic duration. Sparsentan at 100 μmol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration.

Check Digit Verification of cas no

The CAS Registry Mumber 254740-64-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,5,4,7,4 and 0 respectively; the second part has 2 digits, 6 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 254740-64:
(8*2)+(7*5)+(6*4)+(5*7)+(4*4)+(3*0)+(2*6)+(1*4)=142
142 % 10 = 2
So 254740-64-2 is a valid CAS Registry Number.

254740-64-2SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 14, 2017

Revision Date: Aug 14, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-(ethoxymethyl)phenyl]-N-(4,5-dimethyl-1,2-oxazol-3-yl)benzenesulfonamide

1.2 Other means of identification

Product number -
Other names UNII-9242RO5URM

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:254740-64-2 SDS

254740-64-2Downstream Products

254740-64-2Relevant articles and documents

A BIPHENYLSULFONAMIDE ENDOTHELIN AND ANGIOTENSIN II RECEPTOR ANTAGONIST TO TREAT GLOMERULOSCLEROSIS

-

, (2017/07/06)

Methods of administering and pharmaceutical compositions of a biphenyl sulphonamide compound which is a dual angiotensin and endothelin receptor antagonist are disclosed for treating diseases.

BIPHENYL INTERMEDIATE COMPOUNDS AND METHODS FOR THE PREPARATION OF A DUAL ANGIOTENSIN II AND ENDOTHELIN A RECEPTOR ANTAGONIST

-

Page/Page column 22-23, (2010/12/18)

Disclosed herein are methods and compounds useful in preparing N-(3,4-dimethyl-5-isoxazolyl)-2-(4-(2-butyl-4-oxo-l,3-diazospiro[4.4]non-l-en-3yl)methyl-2-ethoxymethylphenyl)phenylsulfonamide.

Dual angiotensin II and endothelin A receptor antagonists: Synthesis of 2′-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics

Murugesan, Natesan,Gu, Zhengxiang,Fadnis, Leena,Tellew, John E.,Baska, Rose Ann F.,Yang, Yifan,Beyer, Sophie M.,Monshizadegan, Hossain,Dickinson, Kenneth E.,Valentine, Maria T.,Humphreys, W. Griffith,Lan, Shih-Jung,Ewing, William R.,Carlson, Kenneth E.,Kowala, Mark C.,Zahler, Robert,Macor, John E.

, p. 171 - 179 (2007/10/03)

In a previous report we demonstrated that merging together key structural elements present in an AT1 receptor antagonist (1, irbesartan) with key structural elements in a biphenylsulfonamide ETA receptor antagonist (2) followed by ad

Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists

-

, (2008/06/13)

Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutica

Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists

-

, (2008/06/13)

Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutica

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