| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Sparsentan (formerly known as PS433540; BMS-346567; RE-021; DARA-a; Filspari) is a novel, highly potent dual antagonist of angiotensin II and endothelin A receptor for the treatment of IgA nephropathy (IgAN). It inhibits the receptors for endothelin A and angiotensin II at concentrations of 0.8 and 9.3 nM, respectively. More and for a longer period of time than DARA 3 or AT(1) or ET(A) receptor antagonists alone, DARA 7 decreased blood pressure elevations in rats brought on by intravenous infusion of Ang II or big ET-1. The combination of AT(1) and ET(A) receptor blockade in a single molecule was demonstrated by Compound 7, which outperformed irbesartan (an AT(1) receptor antagonist) in the normal SHR model of hypertension in a dose-dependent manner. Approved in 2023 by FDA for treating Proteinuria in primary IgA nephropathy.
| Targets |
Human angiotensin II ( Ki = 0.8 nM ); Human endothelin A ( Ki = 9.3 nM ); Rat angiotensin II ( Ki = 0.4 nM )
|
|
|---|---|---|
| ln Vitro |
Sparsentan dose-dependently represses the angiotensin II-induced pressor response with an ED50 value of 0.8 µmol/kg iv and 3.6 µmol/kg po. Sparsentan also demonstrates long-acting and efficacious properties in the large ET-1-induced pressor model. In spontaneously hypertensive rats, sparsentan significantly lowers blood pressure at the lowest dose tested (10 µmol/kg/day). Sparsentan shows good oral bioavailability in rats, dogs, and monkeys, averaging 40%, 86%, and 21% F, respectively. During the course of the drug's pharmacokinetic duration, Sparsentan lowers blood pressure from 170 to less than 100 mmHg at 100 µmol/kg/day. Over the course of its pharmacokinetic duration, sparsentan at 100 µmol/kg/day effectively transforms spontaneously hypertensive rats into normotensive rats[1].
|
|
| ln Vivo |
|
|
| Animal Protocol |
Rats: The first intravenous bolus injection of angiotensin II was administered to the rats as a control pressor response, following their gavage with vehicle. Angiotensin II is given to the rats at different intervals for a maximum of 240 minutes after irbesartan (30 µmol/kg) and sparsentan (30 µmol/kg) are administered orally (po). Every medication dosage involves 6–8 rats. Angiotensin II pressor effect inhibition is expressed as a percentage (%) based on the difference between the maximum blood pressure increase observed before and after the drug [1].
|
|
| References |
| Molecular Formula |
C32H40N4O5S
|
|---|---|
| Molecular Weight |
592.7488
|
| Exact Mass |
592.27
|
| Elemental Analysis |
C, 64.84; H, 6.80; N, 9.45; O, 13.50; S, 5.41
|
| CAS # |
254740-64-2
|
| Related CAS # |
Sparsentan-d5; 1801597-09-0
|
| Appearance |
Solid powder
|
| SMILES |
CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC(=C(C=C3)C4=CC=CC=C4S(=O)(=O)NC5=NOC(=C5C)C)COCC
|
| InChi Key |
WRFHGDPIDHPWIQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35)
|
| Chemical Name |
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
|
| Synonyms |
RE-021; BMS 346567; RE021; Filspari; PS-433540; BMS346567; RE 021; PS 433540; DARA-a; BMS-346567
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~168.7 mM)
Ethanol: ~40 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.51 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6871 mL | 8.4353 mL | 16.8705 mL | |
| 5 mM | 0.3374 mL | 1.6871 mL | 3.3741 mL | |
| 10 mM | 0.1687 mL | 0.8435 mL | 1.6871 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04663204 | Active Recruiting |
Drug: Sparsentan | Kidney Diseases Glomerulonephritis |
University of Leicester | December 10, 2020 | Phase 2 |
| NCT03493685 | Active Recruiting |
Drug: sparsentan Drug: Irbesartan |
Focal Segmental Glomerulosclerosis |
Travere Therapeutics, Inc. | April 17, 2018 | Phase 3 |
| NCT01613118 | Active Recruiting |
Drug: Irbesartan Drug: RE-021 (Sparsentan) |
Focal Segmental Glomerulosclerosis |
Travere Therapeutics, Inc. | March 2014 | Phase 2 |
| NCT03762850 | Active Recruiting |
Drug: sparsentan Drug: irbesartan Drug: Dapagliflozin |
Immunoglobulin A Nephropathy |
Travere Therapeutics, Inc. | December 11, 2018 | Phase 3 |
| NCT05003986 | Recruiting | Drug: Sparsentan | IgA Vasculitis Alport Syndrome |
Travere Therapeutics, Inc. | August 12, 2021 | Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA