254740-64-2 Usage
Description
Sparsentan (PS-433540, RE-021, DARA) is a dual endothelin type A receptor(ETA) and angiotensin II type 1 receptor antagonist.
Uses
RE 201 is used an Endothelin A receptor antagonist used in the treatment of hypertension.
Definition
Sparsentan (RE-021) is a selective dual-acting receptor antagonist with affinity for 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.
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.
254740-64-2Relevant articles and documents
A BIPHENYLSULFONAMIDE ENDOTHELIN AND ANGIOTENSIN II RECEPTOR ANTAGONIST TO TREAT GLOMERULOSCLEROSIS
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Paragraph 0175; 0155; 0157, (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.
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
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, (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
