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
- Molecular Weight:
- 592.75
- MDL Number:
- MFCD16628036
- MOL File:
- 254740-64-2.mol
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 |
FDA UNII | 9242RO5URM |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H315-H319 |
Precautionary statements | P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313 |
Sparsentan (RE-021) price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML2808 | Sparsentan ≥98% (HPLC) | 254740-64-2 | 5MG | $85.3 | 2024-03-01 | Buy |
Sigma-Aldrich | SML2808 | Sparsentan ≥98% (HPLC) | 254740-64-2 | 25MG | $352 | 2024-03-01 | Buy |
TRC | R129300 | RE201 | 254740-64-2 | 1mg | $165 | 2021-12-16 | Buy |
TRC | R129300 | RE201 | 254740-64-2 | 10mg | $1320 | 2021-12-16 | Buy |
Medical Isotopes, Inc. | 72248 | RE201 | 254740-64-2 | 10mg | $2200 | 2021-12-16 | Buy |
Sparsentan (RE-021) Chemical Properties,Uses,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
Sparsentan (RE-021) Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Suzhou Ryan Pharmachem Technology Co.,Ltd. | +86-512-68780025 +8618962125825 | sales@ryanchem.com | China | 137 | 58 |
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 +86-18600796368 | sales@sjar-tech.com | China | 260 | 58 |
Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | admin@nexconn.com | China | 10311 | 58 |
Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 | figo.gao@foxmail.com | China | 7621 | 58 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29823 | 58 |
Nanjing Shizhou Biotechnology Co., Ltd | +86-15850508050 +86-15850508050 | sean.lv@synzest.com | China | 323 | 58 |
ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | eric@witopchemical.com | China | 23555 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10522 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
View Lastest Price from Sparsentan (RE-021) manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2024-09-20 | Sparsentan
254740-64-2
|
US $0.00 / g | 1g | More Than 99% | 100kg/Month | BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | ||
2024-09-19 | Sparsentan
254740-64-2
|
US $0.00-0.00 / Gram | 10Gram | 99 | 5Tons | Chengdu Aupone Pharmaceutical Co.Ltd. | ||
2023-05-08 | Sparsentan
254740-64-2
|
US $0.00-0.00 / g | 100g | 98% | kg grade | Suzhou Ryan Pharmachem Technology Co.,Ltd. |
- Sparsentan
254740-64-2
- US $0.00 / g
- More Than 99%
- BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
- Sparsentan
254740-64-2
- US $0.00-0.00 / Gram
- 99
- Chengdu Aupone Pharmaceutical Co.Ltd.
- Sparsentan
254740-64-2
- US $0.00-0.00 / g
- 98%
- Suzhou Ryan Pharmachem Technology Co.,Ltd.