Sparsentan
- Product Name
- Sparsentan
- CAS No.
- 254740-64-2
- Chemical Name
- Sparsentan
- Synonyms
- Sparsentan;RE-021;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;RE 201;DARA-a;PS433540;Sparentan;BMS-346567;Spashentan;Sparsentan (RE-021)
- CBNumber
- CB12707221
- Molecular Formula
- C32H40N4O5S
- Formula Weight
- 592.75
- MOL File
- 254740-64-2.mol
Sparsentan Property
- 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
- InChI
- InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35)
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- SML2808
- Product name
- Sparsentan
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $85.3
- Updated
- 2024/03/01
- Product number
- SML2808
- Product name
- Sparsentan
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $352
- Updated
- 2024/03/01
- Product number
- R129300
- Product name
- RE201
- Packaging
- 1mg
- Price
- $165
- Updated
- 2021/12/16
- Product number
- R129300
- Product name
- RE201
- Packaging
- 10mg
- Price
- $1320
- Updated
- 2021/12/16
- Product number
- 72248
- Product name
- RE201
- Packaging
- 10mg
- Price
- $2200
- Updated
- 2021/12/16
Sparsentan Chemical Properties,Usage,Production
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.
Sparsentan Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Sparsentan manufacturers
- Product
- Sparsentan 254740-64-2
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-24
- Product
- Sparsentan 254740-64-2
- Price
- US $0.00-0.00/Gram
- Min. Order
- 10Gram
- Purity
- 99
- Supply Ability
- 5Tons
- Release date
- 2024-09-19
- Product
- Sparsentan 254740-64-2
- Price
- US $0.00-0.00/g
- Min. Order
- 100g
- Purity
- 98%
- Supply Ability
- kg grade
- Release date
- 2023-05-08