Sparsentan - CAS 254740-64-2
Catalog number: B0084-475592
Category: Inhibitor
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Molecular Formula:
C32H40N4O5S
Molecular Weight:
592.75
COA:
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Targets:
Angiotensin Receptor | Endothelin Receptor
Description:
Sparsentan, also known as RE-021, BMS346567, is a dual antagonist of both angiotensin II and endothelin A receptor antagonist.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-475592 1 mg $188 In stock
B0084-475592 5 mg $688 In stock
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Purity:
>98%
Appearance:
Solid powder
Synonyms:
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; RE-021; RE021; RE 021; PS-433540; PS433540; PS 433540; DARA-a; Sparsentan
MSDS:
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InChIKey:
WRFHGDPIDHPWIQ-UHFFFAOYSA-N
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)
Canonical SMILES:
CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC(=C(C=C3)C4=CC=CC=C4S(=O)(=O)NC5=NOC(=C5C)C)COCC
1.Interactions between developing autonomic neurons and their target tissues.
Hendry IA;Hill CE;Bonyhady RE Ciba Found Symp. 1981;83:194-212.
Neurons critically depend on contact with the correct target tissue in order to survive and mature. The number of neurons surviving in a nerve centre directly depends on the size of the peripheral field in innervates. It has been proposed that target tissues release a neurotrophic substance (retrophin) which is internalized by nerve terminals and retrogradely transported to the perikarya where its action results in the survival of appropriate neurons. In the sympathetic nervous system, nerve growth factor probably acts as a retrophin. Similar retrophins must exist for other neuronal systems. In order to identify a parasympathetic retrophin two approaches have been taken. One was to grow appropriate target tissues with radiolabelled amino acids and to determine whether the proteins synthesized and released by these target tissues were retrogradely transported by parasympathetic neurons in vivo. The other approach was to show that a purified neurotrophic factor for the chick ciliary ganglion could be retrogradely transported by parasympathetic neurons. The results have suggested that at least two retrophins are involved in the normal development of the autonomic nervous system: one, nerve growth factor, for the sympathetic nervous system and the other, as yet unnamed, for the parasympathetic system.
2.Efficacy and Safety of Sparsentan Compared With Irbesartan in Patients With Primary Focal Segmental Glomerulosclerosis: Randomized, Controlled Trial Design (DUET).
Komers R;Gipson DS;Nelson P;Adler S;Srivastava T;Derebail VK;Meyers KE;Pergola P;MacNally ME;Hunt JL;Shih A;Trachtman H Kidney Int Rep. 2017 Mar 4;2(4):654-664. doi: 10.1016/j.ekir.2017.02.019. eCollection 2017 Jul.
Introduction: ;Primary focal segmental glomerulosclerosis (FSGS) is a leading cause of nephrotic syndrome and end-stage renal disease. There are no US Food and Drug Administration-approved therapies for FSGS, and treatment often fails to reduce proteinuria. Endothelin is an important factor in the pathophysiology of podocyte disorders, including FSGS. Sparsentan is a first-in-class, orally active, dual-acting angiotensin receptor blocker (ARB) and highly selective endothelin Type A receptor antagonist. This study is designed to evaluate whether sparsentan lowers proteinuria compared with an ARB alone and has a favorable safety profile in patients with FSGS.;Methods: ;DUET is a phase 2, randomized, active-control, dose-escalation study with an 8-week, fixed-dose, double-blind period followed by 136 weeks of open-label sparsentan treatment. Patients aged 8 to 75 years with primary FSGS will be randomized to treatment with sparsentan or irbesartan for 8 weeks.;Results: ;The primary efficacy objective is to test the hypothesis that sparsentan over the dose range (200 mg, 400 mg, or 800 mg daily) is superior to irbesartan (300 mg daily) in decreasing the urinary protein-to-creatinine ratio (UPC) from baseline to 8 weeks postrandomization.
3.New drugs and emerging therapeutic targets in the endothelin signaling pathway and prospects for personalized precision medicine.
Davenport AP;Kuc RE;Southan C;Maguire JJ Physiol Res. 2018 Jun 27;67(Supplementum 1):S37-S54.
During the last thirty years since the discovery of endothelin-1, the therapeutic strategy that has evolved in the clinic, mainly in the treatment of pulmonary arterial hypertension, is to block the action of the peptide either at the ET(A) subtype or both receptors using orally active small molecule antagonists. Recently, there has been a rapid expansion in research targeting ET receptors using chemical entities other than small molecules, particularly monoclonal antibody antagonists and selective peptide agonists and antagonists. While usually sacrificing oral bio-availability, these compounds have other therapeutic advantages with the potential to considerably expand drug targets in the endothelin pathway and extend treatment to other pathophysiological conditions. Where the small molecule approach has been retained, a novel strategy to combine two vasoconstrictor targets, the angiotensin AT(1) receptor as well as the ET(A) receptor in the dual antagonist sparsentan has been developed. A second emerging strategy is to combine drugs that have two different targets, the ET(A) antagonist ambrisentan with the phosphodiesterase inhibitor tadalafil, to improve the treatment of pulmonary arterial hypertension.
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CAS 254740-64-2 Sparsentan

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