| Identification | Back Directory | [Name]
Sparsentan (RE-021) | [CAS]
254740-64-2 | [Synonyms]
RE 201
RE-021
PS433540
Sparsentan
BMS-346567
Sparsentan (RE-021)
Sparsentan(PS433540)
formerly known as DARA
Sparsentan-d5 (RE-021-d5)
PS433540; RE-021; FORMERLY KNOWN AS DARA
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
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
[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)- | [Molecular Formula]
C32H40N4O5S | [MDL Number]
MFCD16628036 | [MOL File]
254740-64-2.mol | [Molecular Weight]
592.75 |
| Chemical Properties | Back Directory | [Melting point ]
148 °C(Solv: isopropanol (67-63-0); water (7732-18-5)) | [Boiling point ]
744.4±70.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
7.06±0.50(Predicted) | [color ]
White to off-white | [InChIKey]
WRFHGDPIDHPWIQ-UHFFFAOYSA-N | [SMILES]
C1(C2=CC=C(CN3C(=O)C4(CCCC4)N=C3CCCC)C=C2COCC)=CC=CC=C1S(NC1C(C)=C(C)ON=1)(=O)=O |
| Hazard Information | Back Directory | [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. | [Side effects]
Common side effects of Sparsentan include swelling of the hands, legs, ankles and feet; dizziness; and low red blood cells (anaemia).
Serious side effects of Sparsentan include hives; difficulty breathing; swelling of the face, lips, tongue, or throat; nausea; vomiting; stomach pain (upper right side); tiredness; loss of appetite; yellowing of the skin or eyes (jaundice); dark urine; fever; itching; severe birth defects low blood pressure; dizziness; lightheadedness; fainting; muscle cramps; dry skin; shortness of breath; trouble sleeping; frequent urination; little or no urination; abnormal blood test results (increased potassium); unusual weight gain and swelling of the ankles or legs.
| [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. | [storage]
Store at -20°C |
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