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EP2 ANTAGONIST C52 (C005B-308650)

Catalog No.
C005B-308650
Mfr. No.
SML3643-25MG
Mfr. Name
Sigma-Aldrich
Qty/UOM
1
UOM
EA
Price: $1,152.60
List Price: $1,280.67

Biochem/physiol Actions Compound 52 (C52) is an orally active, brain-penetrant, highly potent and selective prostaglandin E2 (PGE2) receptor 2 (EP2) antagonist (h/r/m EP2 IC50 = 8/10/10 nM against PGE2 binding, IC50 = 5/3/4 nM against 10 nM

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Biochem/physiol Actions

Compound 52 (C52) is an orally active, brain-penetrant, highly potent and selective prostaglandin E2 (PGE2) receptor 2 (EP2) antagonist (h/r/m EP2 IC50 = 8/10/10 nM against PGE2 binding, IC50 = 5/3/4 nM against 10 nM PGE2-induced cellular cAMP) with ∼4000-fold selectivity over other EP receptors (hEP1/3/4 IC50 >30 μM against PGE2 binding; hCRTH2/DP/IP/TP IC50 >33 μM against LTD4-induced cellular Ca2+) and no CYP inhibitory potency. C52 reduces inflammatory neurodegeneration in a murine model of cerebral ischemia (10 mg/kg p.o. 4.5h & 24h post MCAO) and restores cognition in aged mice (10 mg/kg/d p.o.) by rejuvenating cellular bioenergetics in vivo.

UPC:
51142611
Condition:
New
Availability:
3-5 Days
Weight:
1.00 Ounces
HazmatClass:
No
MPN:
SML3643-25MG
CAS:
1799626-16-6

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