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| | SC-51089 Basic information |
| Product Name: | SC-51089 | | Synonyms: | SC-51089;8-Chloro-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic Acid 2-[1-Oxo-3-(4-pyridinyl)propyl]hydrazide Hydrochloride;8-Chloro-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide monohydrochloride;8-Chlorodibenz(Z)[b,f][1,4]oxazepine-10(11H)-carboxylicacid2-[1-oxo-3-(4-pyridinyl)propyl]hydrazidehydrochloride;SC-51089 HCl;Dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 8-chloro-, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide, hydrochloride (1:1) | | CAS: | 146033-02-5 | | MF: | C22H19ClN4O3 | | MW: | 422.86 | | EINECS: | | | Product Categories: | Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer compounds;Pharmaceuticals | | Mol File: | 146033-02-5.mol |  |
| | SC-51089 Chemical Properties |
| Melting point | 162-164°C | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO (25 mg/ml) or water (25 mg/mL) | | form | White solid. | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
| | SC-51089 Usage And Synthesis |
| Description | SC-51089 (146033-02-5) is a prostaglandin E2 (EP1 receptor) antagonist (pA2=6.5, guinea pig ileum muscle strip assay )1,4. Possesses analgesic activity in vivo (rodent ED50= 6.8 mg/kg)1,2,4. SC-51089 does not inhibit COX11 and does not block PGE1 induced hyperalgesia3. | | Chemical Properties | Off-White Solid | | Uses | A selective EP1 prostanoid receptor antagonist that attenuates prostaglandin E2-induced neuronal cell death in vitro and slows tumor growth in vivo. Its neuroprotective effect may potentially have therapeutic application in human stroke. | | Uses | 8-Chloro-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide monohydrochloride is a potent and selective antagonist of EP1 receptors. | | Biological Activity | Selective EP 1 prostanoid receptor antagonist (K i values are 1.3, 11.2, 17.5, 61.1, > 100, > 100, > 100, >100 and > 100 μ M for EP 1 , TP, EP 3 , EP 2 , EP 4 , FP and DP receptors respectively). Attenuates PGE 2 -induced neuronal cell death in vitro and slows tumor growth in vivo . | | References | 1) Hallinan et al. (1993), N-substituted dibenzoxazepines as analgesic PGE2 antagonists; J. Med. Chem., 36
2) Malmberg et al. (1994), Antinociceptive effect of spinally delivered prostaglandin E receptor antagonists in the formalin test on rat; Neurosci. Lett., 173 193
3) Khasar et al. (1994), Comparison of prostaglandin E1- and prostaglandin E2 hyperalgesia in the rat; Neuroscience, 62 345
4) Hallinan et al. (1996), Aminoacetyl moiety as a potential surrogate for diacylhydrazine group of SC-51089, a potent PGE2 antagonist, and its analogs; J. Med. Chem., 39 609 |
| | SC-51089 Preparation Products And Raw materials |
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