LY255283

Modify Date: 2024-01-09 18:50:58

LY255283 Structure
LY255283 structure
Common Name LY255283
CAS Number 117690-79-6 Molecular Weight 360.451
Density 1.2±0.1 g/cm3 Boiling Point 573.4±60.0 °C at 760 mmHg
Molecular Formula C19H28N4O3 Melting Point 160-162 °C
MSDS USA Flash Point 300.6±32.9 °C

 Use of LY255283


LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [3H]LTB4 binding to guinea pig lung membranes[1][2][3][4].

 Names

Name 1-[5-ethyl-2-hydroxy-4-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenyl]ethanone
Synonym More Synonyms

 LY255283 Biological Activity

Description LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [3H]LTB4 binding to guinea pig lung membranes[1][2][3][4].
Related Catalog
Target

LTB4:~100 nM (IC50, LTB4 binds to guinea pig lung membranes)

In Vitro LY255283 compctitively reduces conlractilc responses of lung parcnchyma to LTB, (pA2 = 7.2)[2]. LY255283 (10 μM, 7 days) significantly suppresses the invasiveness of highly aggressive 253 J-BV bladder cancer cells[4]. Cell Viability Assay[4] Cell Line: 253 J-BV cells. Concentration: 5 or 10 μM. Incubation Time: 7 days. Result: Inhibition of BLT2 signaling attenuates aggressive migration by 253 J-BV cells.
In Vivo LY255283 (3, 30 mg/kg) ameliorated lipopolysaccharide-induced ARDS in pigs, possibly by blocking the recruitment of activated PMNs into alveoli in a dose-dependent fashion[3]. LY255283 (2.5 mg/kg, ip) inhibits transitional cell carcinoma metastasis in mice models. The result suggests that a BLT2–Nox–ROS–NF–κB cascade plays a critical role in bladder cancer invasion and metastasis[4]. Animal Model: Mice (253 J-BV cells injected)[4]. Dosage: 2.5 mg/kg. Administration: IP injected 3 and 5 days after injection of cells. Result: By 12 weeks after injection, in mice treated with LY255283 only 0-3 nodules formed per lung, and histological analysis confirmed that the number of micrometastatic lesions was markedly reduced.
References

[1]. R M Schultz, et al. Effects of two leukotriene B4 (LTB4) receptor antagonists (LY255283 and SC-41930) on LTB4-induced human neutrophil adhesion and superoxide production. Prostaglandins Leukot Essent Fatty Acids. 1991 Aug;43(4):267-71.

[2]. S A Silbaugh, et al. Pulmonary actions of LY255283, a leukotriene B4 receptor antagonist. Eur J Pharmacol. 1992 Nov 13;223(1):57-64.

[3]. P S Wollert, et al. LY255283, a novel leukotriene B4 receptor antagonist, limits activation of neutrophils and prevents acute lung injury induced by endotoxin in pigs. Surgery. 1993 Aug;114(2):191-8.

[4]. Eun-Young Kim, et al. BLT2 promotes the invasion and metastasis of aggressive bladder cancer cells through a reactive oxygen species-linked pathway. Free Radic Biol Med. 2010 Sep 15;49(6):1072-81.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 573.4±60.0 °C at 760 mmHg
Melting Point 160-162 °C
Molecular Formula C19H28N4O3
Molecular Weight 360.451
Flash Point 300.6±32.9 °C
Exact Mass 360.216156
PSA 100.99000
LogP 4.04
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.553

 Safety Information

Hazard Codes F+
RIDADR NONH for all modes of transport
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles29

More Articles
Leukotriene B4 Inhibits L-Type Calcium Channels via p38 Signaling Pathway in Vascular Smooth Muscle Cells.

Cell Physiol. Biochem. 37 , 1903-13, (2015)

Arachidonic acid (AA) and its metabolites are important endogenous lipid messengers. In this study, we test the effect of Leukotriene B4 (LTB4), a 5-lipoxygenase metabolite of AA, on L-type calcium ch...

12-Hydroxyheptadecatrienoic acid promotes epidermal wound healing by accelerating keratinocyte migration via the BLT2 receptor.

J. Exp. Med. 211(6) , 1063-78, (2014)

Leukotriene B4 (LTB4) receptor type 2 (BLT2) is a G protein-coupled receptor (GPCR) for 12(S)-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT) and LTB4. Despite the well-defined proinflammatory roles...

A leukotriene B4 receptor-2 is associated with paclitaxel resistance in MCF-7/DOX breast cancer cells.

Br. J. Cancer 109(2) , 351-9, (2013)

Breast cancer is the most common malignancy in women. Although chemotherapeutic agents, such as paclitaxel, are effective treatments for the majority of breast cancer patients, recurrence is frequent ...

 Synonyms

1-(5-Ethyl-2-hydroxy-4-(6-methyl-6-(1H-tetrazol-5-yl)heptyloxy)phenyl)ethanone
1-(5-Ethyl-2-hydroxy-4-{[6-methyl-6-(2H-tetrazol-5-yl)heptyl]oxy}phenyl)ethanone
Ethanone, 1-[5-ethyl-2-hydroxy-4-[[6-methyl-6-(2H-tetrazol-5-yl)heptyl]oxy]phenyl]-
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  • Product Name: LY 255283
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  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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