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Sparsentan

Chemical Structure : Sparsentan

CAS No.: 254740-64-2

Sparsentan (RE-021, DARA-a)

Catalog No.: PC-20515Not For Human Use, Lab Use Only.

Sparsentan (RE-021, DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Ki values of 0.8 and 9.3 nM, respectively.

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Biological Activity

Sparsentan (RE-021, DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Ki values of 0.8 and 9.3 nM, respectively.
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.

Physicochemical Properties

M.Wt 592.76
Formula C32H40N4O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

CCCCC(N(CC1=CC=C(C2=C(S(NC3=NOC(C)=C3C)(=O)=O)C=CC=C2)C(COCC)=C1)C4=O)=NC54CCCC5

References

1. Murugesan N, et al. J Med Chem. 2005 Jan 13;48(1):171-9.

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