SC-51089

SC-51089 is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP1 (Ki = 1.332 µM). It is selective for EP1 over EP2, EP3, and EP4 (Kis = >100, 17.5, and >100 µM, respectively), as well as the PGD2 receptor DP, PGF2alpha receptor FP, PGI2 receptor IP, and thromboxane A2 receptor TP (Kis = >100, 61.13, >100, and 11.18 µM, respectively). SC-51089 (10-50 µM) decreases cell death induced by amyloid-beta 1-42 (Abeta42) in MC65 human neuroblastoma cells. It inhibits the growth of KMG-4 glioma cells in vitro (IC50 = ~1 µM) and reduces tumor growth in a KMG4 mouse xenograft model when administered at a dose of 25 mg/kg. SC-51089 also reduces phenylbenzoquinone-induced writhing in mice (ED50 = 6.8 mg/kg).Formal Name: 8-chloro-2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, monohydrochloride. CAS Number: 146033-02-5. Synonyms: CID-132748. Molecular Formula: C22H19ClN4O3 . HCl. Formula Weight: 459.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. SMILES: O=C(CCc1ccncc1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc12. InChi Code: InChI=1S/C22H19ClN4O3/c23-17-6-7-20-18(13-17)27(14-16-3-1-2-4-19(16)30-20)22(29)26-25-21(28)8-5-15-9-11-24-12-10-15/h1-4,6-7,9-13H,5,8,14H2,(H,25,28)(H,26,29). InChi Key: XDJPQOUDGROSEU-UHFFFAOYSA-N.