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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;Spashentan;Sparsentan (RE-021)
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)
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
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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

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.

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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
ChemScene
Product number
CS-7947
Product name
Sparsentan
Purity
99.08%
Packaging
5mg
Price
$150
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.

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 (RE-021) Preparation Products And Raw materials

Raw materials

Preparation Products

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Sparsentan (RE-021) Suppliers

China 129 India 1 United Kingdom 1 United States 10 Global 141
Suzhou Ryan Pharmaceutical Technology Co., Ltd.
Tel
0512-68780025 18962125825
Email
sales@ryanchem.com
Country
China
ProdList
163
Advantage
62
Anqing Benro pharmachem Technology Co.,Ltd.
Tel
05565209906 15391842992
Email
794263564@qq.com
Country
China
ProdList
116
Advantage
58
Suzhou Albertchem Co.,Ltd.
Tel
0512-88968486 18012631750
Email
sales@albertchemical.com
Country
China
ProdList
285
Advantage
58
Hangzhou Chemtrue Bio-Tech Co.,Ltd.
Tel
0571-86828652 18857119830
Fax
0571-83522824
Email
sales@chemtrue-bio.com
Country
China
ProdList
322
Advantage
58
ChengDu TongChuangYuan Pharmaceutical Co.Ltd
Tel
028-83379370 13880556291
Fax
028-87747383
Email
tcy@tcypharm.com
Country
China
ProdList
6268
Advantage
58
Changzhou Chenhong Biotechnology Co., Ltd.
Tel
0519-85788828 13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
3600
Advantage
58
Chengdu Aupone Pharmaceutical Co.,Ltd.
Tel
18980796919
Email
236656639@qq.com
Country
China
ProdList
23
Advantage
58
Tianjin Hengze Pharmaceutical Technology Co. , Ltd.
Tel
022-20629054 15620629054
Email
ivyding@medhonor.com.cn
Country
China
ProdList
88
Advantage
58
Wuhan HSN Pharmaresearch CO., LTD.
Tel
027-63499089 18086100502
Fax
027-86589137
Email
linwell@126.com
Country
China
ProdList
208
Advantage
50
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
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View Lastest Price from Sparsentan (RE-021) manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
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
Chengdu Aupone Pharmaceutical Co.Ltd.
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
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

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
  • Spashentan
  • 254740-64-2
  • 54740-64-2
  • C32H40N4O5S