LY 255283 | CAS#117690-79-6 | LTB4 Receptor Antagonist

MedKoo Cat#: 525530 | Name: LY 255283

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LY 255283 is a a specific leukotriene B4 (LTB4) receptor antagonist. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.

Chemical Structure

LY 255283

CAS#117690-79-6

Theoretical Analysis

MedKoo Cat#: 525530

Name: LY 255283

CAS#: 117690-79-6

Chemical Formula: C19H28N4O3

Exact Mass: 360.2161

Molecular Weight: 360.46

Elemental Analysis: C, 63.31; H, 7.83; N, 15.54; O, 13.32

Price and Availability

Size	Price	Availability
25mg	USD 350.00	2 weeks
50mg	USD 600.00	2 Weeks
100mg	USD 950.00	2 Weeks

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Related CAS #

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Synonym

LY 255283; LY255283; LY-255283.

IUPAC/Chemical Name

(1-(5-Ethyl-2-hydroxy-4-(6-methyl-6-(1H-tetrazol-5-yl)heptyloxy)phenyl)ethanone)

InChi Key

WCGXJPFHTHQNJL-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H28N4O3/c1-5-14-11-15(13(2)24)16(25)12-17(14)26-10-8-6-7-9-19(3,4)18-20-22-23-21-18/h11-12,25H,5-10H2,1-4H3,(H,20,21,22,23)

SMILES Code

CC(C1=CC(CC)=C(OCCCCCC(C2=NN=NN2)(C)C)C=C1O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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

In vitro activity:

Blockade of BLT2 with the specific antagonist LY255283 or siRNA knockdown significantly suppressed the invasiveness of highly aggressive 253J-BV bladder cancer cells. Reference: Free Radic Biol Med. 2010 Sep 15;49(6):1072-81. https://pubmed.ncbi.nlm.nih.gov/20600831/

In vivo activity:

In control pigs, lipopolysaccharide induced hypoxemia, pulmonary hypertension, and neutrophil activation (increased CORE/MORE ratio). These changes were attenuated by LY255283, particularly when pigs were infused with the higher dose of the compound. Reference: Surgery. 1993 Aug;114(2):191-8. https://pubmed.ncbi.nlm.nih.gov/8393594/

	Solvent	mg/mL	mM
Solubility
	DMF	50.0	138.71
	DMF:PBS (pH 7.2) (1:1)	0.1	0.28
	DMSO	59.5	165.10
	Ethanol	5.0	13.89

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 360.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Kim YR, Park MK, Kang GJ, Kim HJ, Kim EJ, Byun HJ, Lee MY, Lee CH. Leukotriene B4 induces EMT and vimentin expression in PANC-1 pancreatic cancer cells: Involvement of BLT2 via ERK2 activation. Prostaglandins Leukot Essent Fatty Acids. 2016 Dec;115:67-76. doi: 10.1016/j.plefa.2016.10.009. Epub 2016 Nov 3. PMID: 27914516. 2. Kim EY, Seo JM, Kim C, Lee JE, Lee KM, Kim JH. 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. doi: 10.1016/j.freeradbiomed.2010.06.023. Epub 2010 Jun 28. PMID: 20600831. 3. Wollert PS, Menconi MJ, O'Sullivan BP, Wang H, Larkin V, Fink MP. 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. PMID: 8393594. 4. Silbaugh SA, Stengel PW, Cockerham SL, Roman CR, Saussy DL Jr, Spaethe SM, Goodson T Jr, Herron DK, Fleisch JH. Pulmonary actions of LY255283, a leukotriene B4 receptor antagonist. Eur J Pharmacol. 1992 Nov 13;223(1):57-64. doi: 10.1016/0014-2999(92)90818-o. PMID: 1335877.

In vitro protocol:

In vivo protocol:

1. Wollert PS, Menconi MJ, O'Sullivan BP, Wang H, Larkin V, Fink MP. 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. PMID: 8393594. 2. Silbaugh SA, Stengel PW, Cockerham SL, Roman CR, Saussy DL Jr, Spaethe SM, Goodson T Jr, Herron DK, Fleisch JH. Pulmonary actions of LY255283, a leukotriene B4 receptor antagonist. Eur J Pharmacol. 1992 Nov 13;223(1):57-64. doi: 10.1016/0014-2999(92)90818-o. PMID: 1335877.

1: Uğur M, Melli M. Inhibitory effect of LY 255283 on the synthesis of leukotriene B(4) and thromboxane A(2) in human peripheral blood polymorphonuclear leukocytes and monocytes. Mediators Inflamm. 1993;2(6):407-9. PubMed PMID: 18475555; PubMed Central PMCID: PMC2365434.

View History

NSC-80467

MedKoo CAT#: 125767

CAS#: 101982-51-8