Details
Stereochemistry | ACHIRAL |
Molecular Formula | C32H40N4O5S |
Molecular Weight | 592.749 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC(COCC)=C(C=C3)C4=CC=CC=C4S(=O)(=O)NC5=NOC(C)=C5C
InChI
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)
Molecular Formula | C32H40N4O5S |
Molecular Weight | 592.749 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a novel candidate in development by Retrophin for the treatment of focal segmental glomerulosclerosis (FSGS), a serious kidney disorder that often leads to end-stage renal disease (ESRD). Sparsentan is a first-in-class, orally active, dual-acting angiotensin receptor blocker (ARB) and highly selective endothelin Type A receptor antagonist. Sparsentan has been used in trials studying the treatment of focal segmental glomerulosclerosis. The FDA and European Commission have granted sparsentan orphan drug designation for FSGS. Retrophin also is advancing sparsentan for the treatment of immunoglobulin A nephropathy (IgAN) , or Berger’s disease, which also can lead to ESRD. Retrophin is examining the ability of sparsentan to slow the decline of kidney function in patients with FSGS and IgAN.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/29142983
Primary focal segmental glomerulosclerosis (FSGS): oral sparsentan 200 mg, 400 mg, or 800 mg once daily
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15634011
Sparsentan is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 05:42:25 GMT 2023
by
admin
on
Sat Dec 16 05:42:25 GMT 2023
|
Record UNII |
9242RO5URM
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C66930
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
||
|
FDA ORPHAN DRUG |
614417
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
||
|
FDA ORPHAN DRUG |
410113
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
||
|
EU-Orphan Drug |
EU/3/15/1574
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
CHEMBL539423
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
100000163983
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
AB-139
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
SUB178314
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
1304732-86-2
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
NO STRUCTURE GIVEN | |||
|
9242RO5URM
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
254740-64-2
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
DB12548
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
C152412
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
10092
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
9242RO5URM
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY | |||
|
10257882
Created by
admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET -> INHIBITOR |
|
||
|
TARGET -> INHIBITOR |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|