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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
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Product NameSparsentan
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NoteResearch use only, not for human use.
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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.
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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.
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In Vitro——
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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.
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SynonymsRE-021 | DARA-a
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PathwayGPCR/G Protein
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TargetAngiotensin Receptor
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Recptor——
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Research Area——
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Indication——
Chemical Information
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CAS Number254740-64-2
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Formula Weight592.75
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Molecular FormulaC??H??N?O?S
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Purity>98% (HPLC)
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SolubilityDMSO : 250 mg/mL (421.76 mM; Need ultrasonic)；H2O : < 0.1 mg/mL (insoluble)
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SMILES——
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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.
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