| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
KP496 targets the cysteinyl leukotriene receptor 1 (cysLT1, Leukotriene D4 receptor) and the thromboxane A2 receptor (TP). These receptors are involved in inflammatory responses, bronchoconstriction, and platelet aggregation. As a dual antagonist, KP496 blocks the actions of leukotriene D4 and thromboxane A2, thereby reducing inflammation and bronchoconstriction. The compound is a competitive antagonist. Its dual targeting makes it a promising candidate for managing inflammatory conditions, particularly respiratory diseases.
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| ln Vitro |
In vitro, KP496 is a selective, dual antagonist for the Leukotriene D4 receptor and the Thromboxane A2 receptor. As a competitive, dual antagonist, it blocks the actions of both leukotriene D4 and thromboxane A2. Its dual inhibitory activity makes it a valuable tool for studying the roles of these receptors in inflammation and respiratory diseases. The compound's potency and selectivity are typically assessed in receptor binding and functional assays.
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| ln Vivo |
Both acute (day 7) and chronic (day 21) lung inflammation were markedly reduced by KP496. KP496 decreased the amount of neutrophils, eosinophils, macrophages, and lymphocytes on days 7 and 21, as well as on day 7. Prednisolone and KP496 both strongly reduced the rise in the amount of hydroxy-L-proline in the lungs. KP496 and prednisolone decreased the increase in hydroxy-L-proline content by almost 74% and 63%, respectively, when compared to their respective vehicle control groups [1]. The KP496 (100 mg/head) and prednisolone (10 mg/kg) groups considerably reduced the amount of infiltrating lymphocytes, monocytes/macrophages, eosinophils, and total cells when compared to the control group. impact. All cell types except neutrophils had less infiltration in the KP496 (30 mg/head) group, though not to a statistically significant extent [2].
In vivo, KP496 significantly inhibits acute (day 7) and chronic (day 21) lung inflammation. It inhibits epithelial hypertrophy and increases mucus production in asthmatic animals. The compound reduces the infiltration of inflammatory cells, including neutrophils and eosinophils. KP496 is currently in clinical development as a dry powder inhaler, highlighting its potential for treating respiratory inflammatory conditions. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, KP496 is evaluated using radioligand binding studies with membranes expressing the Leukotriene D4 receptor (cysLT1) and the Thromboxane A2 receptor (TP). Competition binding experiments using labeled receptor ligands can determine the compound's affinity for each receptor. Functional assays measuring receptor-mediated signaling, such as calcium mobilization or cAMP modulation, can assess antagonist activity. IC₅0 or Ki values are determined from dose-response curves. Standard assay conditions include physiological buffer systems.
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| Cell Assay |
For in vitro cellular experiments, KP496 is tested in cell lines expressing cysLT1 and TP receptors to evaluate its antagonist activity. Cells are cultured in appropriate media and treated with various concentrations of the compound in the presence of receptor agonists. Receptor activation is measured using calcium-sensitive dyes or other functional readouts. The compound's effects on downstream signaling pathways are further investigated. Its selectivity for cysLT1 and TP over other receptors is assessed.
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| Animal Protocol |
For in vivo animal experiments, KP496 can be administered to rodents via inhalation or other routes to evaluate its anti-inflammatory effects. The compound's efficacy can be evaluated in models of asthma, lung inflammation, or other respiratory diseases. Typical doses may range from 0.1 to 10 mg/kg. Inflammatory markers, lung function, and histological changes are assessed. KP496 significantly inhibits acute and chronic lung inflammation. Animal studies should follow appropriate ethical guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of KP496 are relevant to its clinical development as a dry powder inhaler. As a small molecule with a molecular weight of 692.27, its pharmacokinetic profile would depend on the route of administration. When administered via inhalation, the compound would be delivered directly to the lungs, potentially achieving high local concentrations with reduced systemic exposure. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for KP496 are limited, as it is a research compound in clinical development. As a dual antagonist of inflammatory mediators, its toxicity would depend on the importance of cysLT1 and TP signaling for normal physiological functions. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and respiratory toxicity assessments would be needed for clinical development. Appropriate safety precautions should be taken when handling this compound.
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| References |
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| Additional Infomation |
KP496 is a research compound in clinical development for respiratory inflammation. No regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a selective, dual antagonist for the Leukotriene D4 receptor and Thromboxane A2 receptor that significantly inhibits acute and chronic lung inflammation and is in clinical development as a dry powder inhaler.
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| Molecular Formula |
C31H34CLN3O7S3
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|---|---|
| Molecular Weight |
692.265563488007
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| Exact Mass |
691.124
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| CAS # |
217799-03-6
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| PubChem CID |
11578433
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| Appearance |
White to off-white solid powder
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| LogP |
5.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
45
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| Complexity |
1140
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O)C1=CC=CC=C1S(=O)(N(CCCCNS(=O)(C2=CC=C(Cl)C=C2)=O)CC3=CC=CC(OCC4=NC(C(C)C)=CS4)=C3)=O
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| InChi Key |
WMMCMKVGDPXYQS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H34ClN3O7S3/c1-22(2)28-21-43-30(34-28)20-42-25-9-7-8-23(18-25)19-35(45(40,41)29-11-4-3-10-27(29)31(36)37)17-6-5-16-33-44(38,39)26-14-12-24(32)13-15-26/h3-4,7-15,18,21-22,33H,5-6,16-17,19-20H2,1-2H3,(H,36,37)
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| Chemical Name |
2-[4-[(4-chlorophenyl)sulfonylamino]butyl-[[3-[(4-propan-2-yl-1,3-thiazol-2-yl)methoxy]phenyl]methyl]sulfamoyl]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~144.45 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.61 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 (3.61 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 | 1.4445 mL | 7.2226 mL | 14.4452 mL | |
| 5 mM | 0.2889 mL | 1.4445 mL | 2.8890 mL | |
| 10 mM | 0.1445 mL | 0.7223 mL | 1.4445 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.
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