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Zaloglanstat

CAT: 0804-HY-139589-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-139589-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1

Alternative Products

CatalogName
T39000-01Zaloglanstat

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