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| | LY 171883 Basic information |
| Product Name: | LY 171883 | | Synonyms: | TOMELUKAST;LY-171,833;LY 171883;5-[4-4-ACETYL-3-HYDROXY-2-PROPYLPHENOXYBUTYL]-1H-TETRAZOLE;5-[4-(1-ACETYL-2-HYDROXY-3-PROPYLPHENOXY)BUTYL]-1H-TETRAZOLE;1-[2-HYDROXY-3-PROPYL-4-[4-(1H-TETRAZOL-5-YL)BUTOXY]PHENYL]ETHANONE;1-(2-hydroxy-3-propyl-4-(4-(1h-tetrazol-5-yl)butoxy)phenyl)-ethanon;2’-hydroxy-3’-propyl-4-(4-(1h-tetrazol-5-yl)butoxy)-acetophenon | | CAS: | 88107-10-2 | | MF: | C16H22N4O3 | | MW: | 318.37 | | EINECS: | | | Product Categories: | Prostanoid receptor and related | | Mol File: | 88107-10-2.mol |  |
| | LY 171883 Chemical Properties |
| Melting point | 117-119℃ | | Boiling point | 553.0±60.0 °C(Predicted) | | density | 1.220±0.06 g/cm3(Predicted) | | storage temp. | Store at +4°C | | solubility | Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 15 mg/ml), | | pka | 5.02±0.10(Predicted) | | form | White solid. | | color | White | | Stability: | Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months | | CAS DataBase Reference | 88107-10-2 |
| Hazard Codes | Xn | | Risk Statements | 22 | | Safety Statements | 36 | | WGK Germany | 3 | | RTECS | KM5780800 |
| | LY 171883 Usage And Synthesis |
| Description | LY-171883 (88107-10-2) is a selective and orally active leukotriene D4 (LTD4) antagonist (Ki = 0.63 μM).1 It is also an activator of peroxisome proliferator-activated receptors (PPARs).2,3 | | Uses | LY 171883 is a selective leukotriene D4 antagonist. | | Definition | ChEBI: A member of the class of acetophenones that is 1-phenylethanone substituted at position 2 by a hydroxy group, a propyl group at position 3 and a 4-(1H-tetrazol-5-yl)butoxy group at position 4. A leukotriene antagonist, it exhibits anti
asthmatic activity. | | Biological Activity | Selective, orally active leukotriene D 4 (LTD 4 ) antagonist; inhibits binding of [ 3 H]-LTD 4 to guinea pig lung membranes (K i = 0.63 μ M).? Acts as an agonist at peroxisome proliferator-activated receptors (PPARs). | | in vitro | in gh(3) cells, ly-171883 was able to reversibly increase the amplitude of ca(2+)-activated k(+) current concentration-dependently with an ec(50) value of 15 μm. moreover, the treatment of ly-171883 to cytosolic face did not affect single channel conductance of large-conductance ca(2+)-activated k(+) channels in excised inside-out patches recorded from gh(3) cells, however, ly-171883 did increase the channel activity. in addition, the ly-171883-stimulated activity of bk(ca) channels was dependent on membrane potential [1]. | | in vivo | the effect of ly-171883 on the respiratory and cardiovascular changes in endotoxemia was studied in unanesthetized sheep. in group one, ly-171883 at 4 mg/kg was i.v. injected. in group two, escherichia coli endotoxin (1 μg/kg) was infused, and in group three, ly-171883 at 4 mg/kg was administered before and after the same dose of endotoxin. results showed that infusion of ly-171883 in group one did not alter baseline ventilatory and cardiovascular measurements. in group two, a two-phase pulmonary response was found. an early pulmonary hypertension phase with a fall in cardiac index was observed in group three [2]. | | References | 1) Fleisch et al. (1985), LY171883, 1-less than 2-hydroxy-3-propyl-4-less than 4-(1H-tetrazol-5-yl)butoxy greater than phenyl greater than ethanone, an orally active leukotriene D4 antagonist; J. Pharmacol. Exp. Ther., 233 148
2) Foxworthy and Eacho (1991) Effect of the peroxisome proliferator LY171883 on triglyceride accumulation in rats fed a fat-free diet; Biochem. Pharmacol. 42 1487
3) Kliewer et al. (1994) Differential expression and activation of a family of murine peroxisome proliferator-activated receptors; Proc. Natl. Acad. Sci .USA 91 7355 |
| | LY 171883 Preparation Products And Raw materials |
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