LY 223982 | CAS#117423-74-2 | BLT1 Receptor Antagonist

LY 223982
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525522

CAS#: 117423-74-2

Description: LY 223982 is a potent BLT1 receptor antagonist. It inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM. LY223982 inhibits the leukotriene B4 (LTB4)-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.

Chemical Structure

LY 223982

CAS# 117423-74-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525522
Name: LY 223982
CAS#: 117423-74-2
Chemical Formula: C30H30O7
Exact Mass: 502.20
Molecular Weight: 502.563
Elemental Analysis: C, 71.70; H, 6.02; O, 22.28

Price and Availability

Size	Price	Availability
5mg	USD 350	2 weeks
10mg	USD 600	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: LY 223982; LY-223982; LY223982.

IUPAC/Chemical Name: 5-(3-Carboxybenzoyl)-2-((6-(4-methoxyphenyl)-5-hexenyl)oxy)benzenepropanoic acid

InChi Key: SYZSSLLFRVDRHL-QPJJXVBHSA-N

InChi Code: InChI=1S/C30H30O7/c1-36-26-14-10-21(11-15-26)7-4-2-3-5-18-37-27-16-12-24(19-22(27)13-17-28(31)32)29(33)23-8-6-9-25(20-23)30(34)35/h4,6-12,14-16,19-20H,2-3,5,13,17-18H2,1H3,(H,31,32)(H,34,35)/b7-4+

SMILES Code: O=C(O)CCC1=CC(C(C2=CC=CC(C(O)=O)=C2)=O)=CC=C1OCCCC/C=C/C3=CC=C(OC)C=C3

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:

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Biological target:	LY223982 is a potent and specific inhibitor of leukotriene B4 receptor, with an IC50 of 13.2 nM against [3H]LTB4 binding to LTB4 receptor.
In vitro activity:	5-Oxo-ETE was isolated from the alkaline hydrolysis products of LTA(4) in order to evaluate its effects on human polymorphonuclear (PMN) leukocytes. Pretreatment of the cells with LTB(4) totally abolished the calcium response induced by 5-oxo-ETE. In contrast, the preincubation with 5-oxo-ETE did not affect the calcium mobilization induced by LTB(4). The calcium response induced by 5-oxo-ETE was totally inhibited by the specific LTB(4) receptor antagonist LY223982. Reference: Biochim Biophys Acta. 2000 Feb 24;1484(1):51-8. https://pubmed.ncbi.nlm.nih.gov/10685030/
In vivo activity:	LY223982, (E)-5-(3-carboxybenzoyl)-2-((6-(4-methoxyphenyl)-5- hexenyl)oxy)benzenepropanoic acid, is a newly discovered potent inhibitor of specific binding of leukotriene B4 (LTB4) to its receptor on human neutrophils.This study demonstrated that the compound is also a specific antagonist of LTB4-induced neutrophil activation under both in vitro and in vivo conditions. LY223982 inhibited transient leukopenia induced in rabbits with LTB4 (ED50, 3 mg/kg) but not with FMLP. Reference: J Pharmacol Exp Ther. 1992 Dec;263(3):1009-14. https://pubmed.ncbi.nlm.nih.gov/1335049/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	30.0	59.69
	DMF:PBS (pH 7.2) (1:1)	0.5	0.99
	DMSO	60.0	119.39
	Ethanol	0.1	0.20

Preparing Stock Solutions

The following data is based on the product molecular weight 502.56 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. Falgueyret J, Riendeau D. LTA(4)-derived 5-oxo-eicosatetraenoic acid: pH-dependent formation and interaction with the LTB(4) receptor of human polymorphonuclear leukocytes. Biochim Biophys Acta. 2000 Feb 24;1484(1):51-8. doi: 10.1016/s1388-1981(99)00198-5. PMID: 10685030. 2. Rainger GE, Rowley AF, Nash GB. Adhesion-dependent release of elastase from human neutrophils in a novel, flow-based model: specificity of different chemotactic agents. Blood. 1998 Dec 15;92(12):4819-27. PMID: 9845549. 3. Jackson WT, Boyd RJ, Froelich LL, Mallett BE, Gapinski DM. Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982. J Pharmacol Exp Ther. 1992 Dec;263(3):1009-14. PMID: 1335049. 4. Griswold DE, Martin L, Ventre J, Meunier L, Perry L. Technique for quantification of LTB4-induced changes in peripheral granulocyte counts in vivo in the rabbit. J Pharmacol Methods. 1991 Jul;25(4):319-28. doi: 10.1016/0160-5402(91)90031-y. PMID: 1653383.
In vitro protocol:	1. Falgueyret J, Riendeau D. LTA(4)-derived 5-oxo-eicosatetraenoic acid: pH-dependent formation and interaction with the LTB(4) receptor of human polymorphonuclear leukocytes. Biochim Biophys Acta. 2000 Feb 24;1484(1):51-8. doi: 10.1016/s1388-1981(99)00198-5. PMID: 10685030. 2. Rainger GE, Rowley AF, Nash GB. Adhesion-dependent release of elastase from human neutrophils in a novel, flow-based model: specificity of different chemotactic agents. Blood. 1998 Dec 15;92(12):4819-27. PMID: 9845549.
In vivo protocol:	1. Jackson WT, Boyd RJ, Froelich LL, Mallett BE, Gapinski DM. Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982. J Pharmacol Exp Ther. 1992 Dec;263(3):1009-14. PMID: 1335049. 2. Griswold DE, Martin L, Ventre J, Meunier L, Perry L. Technique for quantification of LTB4-induced changes in peripheral granulocyte counts in vivo in the rabbit. J Pharmacol Methods. 1991 Jul;25(4):319-28. doi: 10.1016/0160-5402(91)90031-y. PMID: 1653383.

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1: Lee W, Su Kim H, Lee GR. Leukotrienes induce the migration of Th17 cells. Immunol Cell Biol. 2015 May-Jun;93(5):472-9. doi: 10.1038/icb.2014.104. Epub 2014 Dec 16. PubMed PMID: 25512344.

2: Falgueyret J, Riendeau D. LTA(4)-derived 5-oxo-eicosatetraenoic acid: pH-dependent formation and interaction with the LTB(4) receptor of human polymorphonuclear leukocytes. Biochim Biophys Acta. 2000 Feb 24;1484(1):51-8. PubMed PMID: 10685030.

3: Feng Z, Godfrey HP, Mandy S, Strudwick S, Lin KT, Heilman E, Wong PY. Leukotriene B4 modulates in vivo expression of delayed-type hypersensitivity by a receptor-mediated mechanism: regulation by lipoxin A4. J Pharmacol Exp Ther. 1996 Aug;278(2):950-6. PubMed PMID: 8768752.

4: Jackson WT, Boyd RJ, Froelich LL, Gapinski DM, Mallett BE, Sawyer JS. Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists. J Med Chem. 1993 Jun 11;36(12):1726-34. PubMed PMID: 8389876.

5: Rediske J, Morrissey MM, Jarvis M. Human monocytes respond to leukotriene B4 with a transient increase in cytosolic calcium. Cell Immunol. 1993 Apr 1;147(2):438-45. PubMed PMID: 8384085.

6: Jackson WT, Boyd RJ, Froelich LL, Mallett BE, Gapinski DM. Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982. J Pharmacol Exp Ther. 1992 Dec;263(3):1009-14. PubMed PMID: 1335049.

7: McDonald PP, McColl SR, Naccache PH, Borgeat P. Activation of the human neutrophil 5-lipoxygenase by leukotriene B4. Br J Pharmacol. 1992 Sep;107(1):226-32. PubMed PMID: 1330161; PubMed Central PMCID: PMC1907591.

8: Jackson RH, Morrissey MM, Sills MA, Jarvis MF. Comparison of antagonist and agonist binding to the leukotriene B4 receptor intact human polymorphonuclear neutrophils (PMN). J Pharmacol Exp Ther. 1992 Jul;262(1):80-9. PubMed PMID: 1320692.

9: Moreira-Ludewig R, Healy CT. A rapid microtiter plate method for the detection of lysozyme release from human neutrophils. J Pharmacol Toxicol Methods. 1992 Apr;27(2):95-100. PubMed PMID: 1317227.

10: Li EJ, Cook JA, Wise WC, Jackson WT, Halushka PV. Effect of LTB4 receptor antagonists in endotoxic shock in the rat. Circ Shock. 1991 Aug;34(4):385-92. PubMed PMID: 1663429.

11: Griswold DE, Martin L, Ventre J, Meunier L, Perry L. Technique for quantification of LTB4-induced changes in peripheral granulocyte counts in vivo in the rabbit. J Pharmacol Methods. 1991 Jul;25(4):319-28. PubMed PMID: 1653383.

12: Turner CR, Lackey MN, Quinlan MF, Griswold DE, Schwartz LW, Wheeldon EB. Therapeutic intervention in a rat model of adult respiratory distress syndrome: II. Lipoxygenase pathway inhibition. Circ Shock. 1991 Jun;34(2):263-9. PubMed PMID: 1934327.

13: Psychoyos S, Uziel-Fusi S, Morrissey MM, Ganu V, Smith CW. Thick filter neutrophil chemotaxis performed in the absence of albumin. J Immunol Methods. 1991 Mar 1;137(1):37-46. PubMed PMID: 1849155.

14: Gapinski DM, Mallett BE, Froelich LL, Jackson WT. Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain. J Med Chem. 1990 Oct;33(10):2807-13. PubMed PMID: 2170648.

15: Downey GP, Chan CK, Trudel S, Grinstein S. Actin assembly in electropermeabilized neutrophils: role of intracellular calcium. J Cell Biol. 1990 Jun;110(6):1975-82. PubMed PMID: 2112547; PubMed Central PMCID: PMC2116117.

16: Mong S, Votta B, Sarau HM, Foley JJ, Schmidt D, Carte BK, Poehland B, Westley J. 15-Acetylthioxy-furodysinin lactone, isolated from a marine sponge Dysidea, sp. is a potent agonist to human leukotriene B4 receptor. Prostaglandins. 1990 Jan;39(1):89-97. PubMed PMID: 2155439.

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