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MedKoo Cat#: 525522 | Name: LY 223982
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Description:

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

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
LY 223982
CAS#117423-74-2

Theoretical Analysis

MedKoo Cat#: 525522

Name: LY 223982

CAS#: 117423-74-2

Chemical Formula: C30H30O7

Exact Mass: 502.1992

Molecular Weight: 502.56

Elemental Analysis: C, 71.70; H, 6.02; O, 22.28

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 weeks
10mg USD 600.00 2 weeks
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No Data
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
View handling instruction
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/
Solvent mg/mL 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
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 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.

Recalculate based on batch purity %
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.
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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NSC-80467

NSC-80467