Zaloglanstat (ISC-27864, GRC-27864)

Chemical Structure : Zaloglanstat

CAS No.: 1513852-12-4

Catalog No.: PC-38688Not For Human Use, Lab Use Only.

Zaloglanstat (ISC-27864, GRC-27864) is a potent, selective, non-opioid and orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50 of 5 nM (human mPGES-1).

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5 mg	$278	In stock
10 mg	$458	In stock
25 mg	$728	In stock
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Biological Activity

Zaloglanstat (ISC-27864, GRC-27864) is a potent, selective, non-opioid and orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50 of 5 nM (human mPGES-1).

Zaloglanstat (ISC-27864, GRC-27864) shows no significant inhibitory effect on COX-1/2.

Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s of 161 nM and 154 nM, respectively.

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 exhibits significant analgesic efficacy in preclinical models for osteoarthritis and inflammatory arthritis.

Physicochemical Properties

M.Wt	452.862
Formula	C21H20ClF3N4O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-2,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl)pivalamide

References

1. Sant S, et al. Osteoarthritis Cartilage 2018, 26, S351– S352, DOI: 10.1016/j.joca.2018.02.698