ChemicalBook > CAS DataBase List > Sparsentan (RE-021)

Sparsentan (RE-021)

Product Name
Sparsentan (RE-021)
CAS No.
254740-64-2
Chemical Name
Sparsentan (RE-021)
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;Sparsentan (RE-021);Sparsentan(PS433540)
CBNumber
CB12707221
Molecular Formula
C32H40N4O5S
Formula Weight
592.75
MOL File
254740-64-2.mol
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Sparsentan (RE-021) 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)
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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

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.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2808
Product name
Sparsentan
Purity
≥98% (HPLC)
Packaging
5MG
Price
$85.3
Updated
2024/03/01
Sigma-Aldrich
Product number
SML2808
Product name
Sparsentan
Purity
≥98% (HPLC)
Packaging
25MG
Price
$352
Updated
2024/03/01
TRC
Product number
R129300
Product name
RE201
Packaging
1mg
Price
$165
Updated
2021/12/16
TRC
Product number
R129300
Product name
RE201
Packaging
10mg
Price
$1320
Updated
2021/12/16
Medical Isotopes, Inc.
Product number
72248
Product name
RE201
Packaging
10mg
Price
$2200
Updated
2021/12/16
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Sparsentan (RE-021) 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.

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 (RE-021) Preparation Products And Raw materials

Raw materials

Preparation Products

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Sparsentan (RE-021) Suppliers

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View Lastest Price from Sparsentan (RE-021) manufacturers

Suzhou Ryan Pharmachem Technology Co.,Ltd.
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
Career Henan Chemical Co
Product
Sparsentan (RE-021) 254740-64-2
Price
US $6.68/KG
Min. Order
1KG
Purity
97%-99%
Supply Ability
1kg-1000kg
Release date
2020-01-09

254740-64-2, Sparsentan (RE-021)Related Search:

Isobutylbenzene 2-Chloro-2-methylpropane 4-Methyl-2-pentanone

  • 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
  • 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
  • BMS-346567
  • 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
  • formerly known as DARA
  • PS433540
  • PS433540; RE-021; FORMERLY KNOWN AS DARA
  • RE-021
  • Sparsentan(PS433540)
  • 4'-[(2-Butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-...
  • DARA-a
  • Sparsentan,RE 021,Inhibitor,inhibit,Angiotensin Receptor,Endothelin Receptor,RE021
  • Sparentan
  • 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
  • 254740-64-2
  • 54740-64-2
  • C32H40N4O5S