Zaloglanstat

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].

Product Specifications

CAS Number

[1513852-12-4]

Product Name Alternative

ISC-27864; GRC-27864

UNSPSC

12352005

Target

Collagen; COX; PGE synthase

Type

Reference compound

Related Pathways

Cytoskeleton; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/zaloglanstat.html

Purity

98.50

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C1NC(C2=C(Cl)C=CC(CNC(C(C)(C)C)=O)=C2)=NN1C3=CC=C(C(F)(F)F)C=C3

Molecular Formula

C21H20ClF3N4O2

Molecular Weight

452.86

References & Citations

[1]Zhang YY, et al. Microsomal prostaglandin E2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance. Pharmacol Res. 2022 Jan;175:105977.|[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.|[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.