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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;Spasentan;BMS-346567;Spashentan
CBNumber
CB12707221
Molecular Formula
C32H40N4O5S
Formula Weight
592.75
MOL File
254740-64-2.mol
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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
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Safety

WGK Germany 
WGK 3
Storage Class
11 - Combustible Solids
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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
$83.31
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2808
Product name
Sparsentan
Purity
≥98% (HPLC)
Packaging
25MG
Price
$362
Updated
2025/07/31
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 Chemical Properties,Usage,Production

Description

Sparsentan is an oral, dual endothelin angiotensin receptor antagonist that is being developed by Travere Therapeutics for the treatment of immunoglobulin A (IgA) nephropathy and focal segmental glomerulosclerosis (FSGS).[1]

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.

References

[1] Syed, Yahiya Y. “Sparsentan: First Approval.” Drugs 83 6 (2023): 563–568.

Sparsentan Preparation Products And Raw materials

Raw materials

Preparation Products

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Sparsentan Suppliers

Suzhou Ryan Pharmaceutical Technology Co., Ltd.
Tel
0512-68780025 18962125825
Email
sales@ryanchem.com
Country
China
ProdList
168
Advantage
62
Anqing Benro pharmachem Technology Co.,Ltd.
Tel
05565209906 15391842992
Email
794263564@qq.com
Country
China
ProdList
126
Advantage
58
Hangzhou Chemtrue Bio-Tech Co.,Ltd.
Tel
0571-86828652 18857119830
Fax
0571-83522824
Email
sales@chemtrue-bio.com
Country
China
ProdList
258
Advantage
58
ChengDu TongChuangYuan Pharmaceutical Co.Ltd
Tel
028-83379370 13880556291
Fax
028-87747383
Email
tcy@tcypharm.com
Country
China
ProdList
7220
Advantage
58
Changzhou Chenhong Biotechnology Co., Ltd.
Tel
+86-0519-85788828 +86-13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
4023
Advantage
58
Chengdu Aupone Pharmaceutical Co.,Ltd.
Tel
18980796919; 18980796919
Email
236656639@qq.com
Country
China
ProdList
29
Advantage
58
Tianjin Zhennuo Pharmaceutical Group Co., Ltd
Tel
15620629054
Email
ivyding@medhonor.com.cn
Country
China
ProdList
64
Advantage
58
Jurong Coupling Biotechnology Co., Ltd.
Tel
19231718652
Email
278191416@qq.com
Country
China
ProdList
480
Advantage
58
Shenzhen Yaoyuan R&D Center Co., Ltd
Tel
23284190 13421666688
Email
664261110@qq.com
Country
China
ProdList
83
Advantage
58
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 manufacturers

Shaanxi Dideu New Materials Co. Ltd
Product
Sparsentan 254740-64-2
Price
US $0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1000kg
Release date
2025-11-17
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

254740-64-2, Sparsentan Related Search:


  • 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
  • Spashentan
  • Sparsentan, 10 mM in DMSO
  • Sparsentan (PS-433540, RE-021)
  • Spasentan
  • 254740-64-2
  • 54740-64-2
  • C32H40N4O5S
  • API