An mPGES-1 inhibitor
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Prostaglandin E2 Inhibitor 3

Item No. 38316

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-bromo-N-[5-(3′-hydroxy[1,1′-biphenyl]-4-yl)-1,3,4-thiadiazol-2-yl]-benzamide
CAS Number
3054217-03-4
Synonyms
  • PGE2 Inhibitor 3
Molecular Formula
C21H14BrN3O2S
Formula Weight
452.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleEthanol: Soluble
SMILES
O=C(C1=CC=CC=C1Br)NC2=NN=C(C3=CC=C(C4=CC(O)=CC=C4)C=C3)S2
InChi Code
InChI=1S/C21H14BrN3O2S/c22-18-7-2-1-6-17(18)19(27)23-21-25-24-20(28-21)14-10-8-13(9-11-14)15-4-3-5-16(26)12-15/h1-12,26H,(H,23,25,27)
InChi Key
WRBRJSBQVMFDGA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Prostaglandin E2 (PGE2) inhibitor 3 is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM).1 It is selective for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in cell-free assays at 10 µM. PGE2 inhibitor 3 inhibits IL-1β-induced production of PGE2 (Item No. 14010) in A549 cells and LPS-induced IL-6 and PGE2 production in J774A.1 macrophages when used at concentrations of 10 and 1 µM, respectively. It also inhibits the formation of 5-LO products, including leukotriene B4 (LTB4; Item No. 20110) and 5-H(p)ETE, induced by the calcium ionophore A23187 (Item Nos. 11016 | 22030) alone or with arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) and A23187 (IC50s = 4.9 and 5.2 µM, respectively). In vivo, PGE2 inhibitor 3 (10 mg/kg) prevents leukocyte infiltration into the peritoneal fluid in a mouse model of zymosan-induced peritonitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Potenza, M., Giodano, A., Chini, M.G., et al. Identification of 2-aminoacyl-1,3,4-thiadiazoles as prostaglandin E2 and leukotriene biosynthesis inhibitors. ACS Med. Chem. Lett. 14(1), 26-34 (2023).