1. GPCR/G Protein
  2. Angiotensin Receptor
    Endothelin Receptor

Sparsentan (Synonyms: RE-021; DARA-a)

Cat. No.: HY-17621 Purity: 99.08%
Handling Instructions

Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.

For research use only. We do not sell to patients.

Sparsentan Chemical Structure

Sparsentan Chemical Structure

CAS No. : 254740-64-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1017 In-stock
Estimated Time of Arrival: December 31
1 mg USD 228 In-stock
Estimated Time of Arrival: December 31
5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2340 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5640 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.

IC50 & Target

Ki: 0.8 nM (Human angiotensin II), 9.3 nM (Human endothelin A), 0.4 nM (Rat angiotensin II)[1]

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[1].

Clinical Trial
References
Animal Administration
[1]

Rats: Rats are gavaged with vehicle, and immediately thereafter the first bolus (intravenous) iv injection of angiotensin II served as the control pressor response. Irbesartan (30 µmol/kg) and Sparsentan (30 µmol/kg) are given by oral gavage (po), and the rats are re-challenged with angiotensin II at various intervals up to 240 min. There are 6-8 rats per drug dose. The difference between the maximum blood pressure increase before and after drug is reported as the percent (%) inhibition of the angiotensin II pressor effect[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

592.75

Formula

C₃₂H₄₀N₄O₅S

CAS No.

254740-64-2

SMILES

O=S(C1=CC=CC=C1C2=CC=C(CN3C(CCCC)=NC4(CCCC4)C3=O)C=C2COCC)(NC5=NOC(C)=C5C)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Sparsentan
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HY-17621
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Sparsentan

Cat. No.: HY-17621