1513852-12-4
Chemical Structure
Zaloglanstat
Synonym(s): ISC-27864; GRC-27864
- CAS No.: 1513852-12-4
- Formula:C21H20ClF3N4O2
- Molecular Weight:452.86
IUPAC Name: N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl)pivalamide
InChIKey: DOVBVLUPCQSAGE-UHFFFAOYSA-N
SMILES: O=C1NC(C2=C(Cl)C=CC(CNC(C(C)(C)C)=O)=C2)=NN1C3=CC=C(C(F)(F)F)C=C3
Biological Activity: Zaloglanstat (ISC-27864; GRC-27864) is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC50 of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 (IC50 >10 μM). Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Zaloglanstat | 98.50% | Zaloglanstat (ISC-27864; GRC-27864) is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC50 of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 (IC50 >10 μM). Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Zhang YY, et al. Microsomal prostaglandin E2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance. Pharmacol Res. 2022 Jan;175:105977. [Content Brief]
- [2]. Di Micco S, et al. Identification of 2-(thiophen-2-yl)acetic Acid-Based Lead Compound for mPGES-1 Inhibition. Front Chem. 2021 May 7;9:676631. [Content Brief]
- [3]. Mann MK, et al. Structure-Activity Relationship of USP5 Inhibitors [published correction appears in J Med Chem. 2022 Jan 13;65(1):889]. J Med Chem. 2021;64(20):15017-15036. [Content Brief]
Keywords
