| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
LY223982 targets the leukotriene B₄ (LTB₄) receptor, specifically the BLT1 receptor (also known as P2Y7). LTB₄ is a potent chemoattractant and pro-inflammatory lipid mediator that plays a critical role in neutrophil recruitment and activation. LY223982 is a potent and selective antagonist with an IC50 of 13.2 nM for inhibition of [³H]LTB₄ binding.
|
|---|---|
| ln Vitro |
LY223982 is a leukotriene B4 (LTB4) receptor inhibitor that is both strong and selective. Its IC50 for [3H]LTB4 binding to the LTB4 receptor is 13.2 nM. Additionally, LY223982 is a strong inhibitor (IC50, 100 nM) of the recruitment of human neutrophils produced by LTB4 [1].
In vitro, LY223982 inhibits the specific binding of radiolabeled LTB₄ to isolated human neutrophils with an IC50 of 13.2 nM. The compound is a potent and selective LTB₄ receptor antagonist that blocks LTB₄-induced neutrophil activation and transient leukopenia. By antagonizing the LTB₄ receptor, the compound inhibits LTB₄-mediated chemotaxis, degranulation, and superoxide production in neutrophils. |
| ln Vivo |
Inhibiting LTB4 (ED50, 3 mg/kg)-induced transient leukopenia in rabbits, LY223982 does not exhibit agonist activity in any of the tested systems and does not block FMLP [1].
In vivo, LY223982 has been studied for its anti-inflammatory properties. As a potent LTB₄ receptor antagonist, it has the potential to inhibit LTB₄-mediated inflammatory responses, including neutrophil recruitment and activation. The compound's ability to block LTB₄-induced transient leukopenia supports its role in modulating inflammatory processes. |
| Enzyme Assay |
In vitro receptor binding assays for LTB₄ receptor antagonism involve incubating isolated human neutrophils or membranes from cells expressing the BLT1 receptor with [³H]LTB₄ and varying concentrations of LY223982. Non-specific binding is determined using excess unlabeled LTB₄. The reaction is terminated by rapid filtration, and bound radioactivity is measured by scintillation counting to calculate IC50 values.
|
| Cell Assay |
Cellular assays are performed using isolated human neutrophils or cell lines expressing the BLT1 receptor. Cells are treated with LY223982 at various concentrations and then stimulated with LTB₄. Chemotaxis is measured using Boyden chamber or transwell assays. Neutrophil activation is assessed by measuring superoxide production, degranulation, or calcium mobilization. The inhibition of LTB₄-induced responses confirms receptor antagonism.
|
| Animal Protocol |
In vivo studies are conducted in animal models of inflammation, such as carrageenan-induced paw edema or LPS-induced lung inflammation. LY223982 is administered intraperitoneally or orally at various doses. Inflammatory markers and neutrophil infiltration are assessed in tissues. Transient leukopenia induced by LTB₄ administration may be used as a pharmacodynamic endpoint.
|
| ADME/Pharmacokinetics |
LY223982 (molecular weight 502.56, formula C₃₀H₃₀O₇) is a small-molecule compound. It is a benzophenone dicarboxylic acid derivative with a purity of ≥95%. The compound is soluble in DMSO and is typically stored at -20°C. Its physicochemical properties support its use in both in vitro and in vivo studies.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity studies have evaluated LY223982 in animal models. As an LTB₄ receptor antagonist, its toxicity profile is related to modulation of inflammatory responses. No significant toxicity has been reported at therapeutic doses. The compound's safety profile supports its use in research applications.
|
| References | |
| Additional Infomation |
LY223982 is a potent and selective LTB₄ receptor antagonist developed for studying inflammatory processes. Its mechanism involves blocking the LTB₄ receptor, inhibiting LTB₄-mediated neutrophil chemotaxis, activation, and inflammatory responses. The compound is a benzophenone dicarboxylic acid derivative that has been used as a research tool to investigate the role of LTB₄ in inflammation and immune responses. LY223982 has not received regulatory approval for clinical use.
|
| Molecular Formula |
C30H30O7
|
|---|---|
| Molecular Weight |
502.555
|
| Exact Mass |
502.199
|
| CAS # |
117423-74-2
|
| PubChem CID |
6444688
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
753.8±60.0 °C at 760 mmHg
|
| Flash Point |
248.4±26.4 °C
|
| Vapour Pressure |
0.0±2.7 mmHg at 25°C
|
| Index of Refraction |
1.612
|
| LogP |
6.32
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
37
|
| Complexity |
755
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC=C(C=C1)/C=C/CCCCOC2=C(C=C(C=C2)C(=O)C3=CC(=CC=C3)C(=O)O)CCC(=O)O
|
| 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+
|
| Chemical Name |
5-(3-Carboxybenzoyl)-2-((6-(4-methoxyphenyl)-5-hexenyl)oxy)benzenepropanoic acid
|
| Synonyms |
LY 223982; LY-223982; LY223982.
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~198.98 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9898 mL | 9.9491 mL | 19.8981 mL | |
| 5 mM | 0.3980 mL | 1.9898 mL | 3.9796 mL | |
| 10 mM | 0.1990 mL | 0.9949 mL | 1.9898 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA