Cart
sales@molnova.com
Sparsentan
CAS No. 254740-64-2
Sparsentan( RE-021 | DARA-a )
Catalog No. M21831 CAS No. 254740-64-2
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.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 70 | In Stock |
|
| 5MG | 113 | In Stock |
|
| 10MG | 165 | In Stock |
|
| 25MG | 267 | In Stock |
|
| 50MG | 410 | In Stock |
|
| 100MG | 602 | In Stock |
|
| 500MG | 1278 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NameSparsentan
-
NoteResearch use only, not for human use.
-
Brief DescriptionSparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
-
DescriptionSparsentan (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 Vivo):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.
-
In Vitro——
-
In VivoSparsentan 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.
-
SynonymsRE-021 | DARA-a
-
PathwayGPCR/G Protein
-
TargetAngiotensin Receptor
-
Recptor——
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number254740-64-2
-
Formula Weight592.75
-
Molecular FormulaC??H??N?O?S
-
Purity>98% (HPLC)
-
SolubilityDMSO : 250 mg/mL (421.76 mM; Need ultrasonic)；H2O : < 0.1 mg/mL (insoluble)
-
SMILES——
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Murugesan N, et al. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.
molnova catalog
related products
-
Candesartan cilexeti...
An angiotensin II receptor antagonist used mainly for the treatment of hypertension.
-
Norleual
Angiotensin IV analog. Highly potent HGF/c-MET inhibitor (IC50 = 3 pM). Inhibits HGF-induced MDCK cell proliferation and invasion in vitro. Also AT4 receptor antagonist; disrupts LTP stabilization. Antiangiogenic.
-
C-Type Natriuretic P...
CNP, a member of the natriuretic peptide family, was first identified in porcine brain and later found in other mammals as well as non-mammals. Processing of the CNP precursor gives rise to CNP-22 and its N-terminally elongated form, CNP-53. The CNPs share considerable sequence homology with ANP and BNP within the disulfide loop and exert similar pharmacological actions, although with different relative potencies.
