| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
SR 2640 hydrochloride is a potent and selective competitive antagonist of leukotriene D4 (LTD4) and leukotriene E4 (LTE4) receptors. By blocking these receptors, it inhibits the actions of leukotrienes, which are inflammatory mediators involved in asthma and other inflammatory conditions. Its mechanism involves competitive antagonism at the leukotriene D4 and E4 receptors. SR 2640 can be used to study the role of leukotrienes in human asthma.
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| ln Vitro |
In vitro, SR 2640 hydrochloride inhibits LTD4- but not histamine-induced guinea pig ileum and trachea contraction, with a pA2 of 8.7. Its in vitro activity is characterized by potent and selective antagonism of leukotriene D4 and E4 receptors. The compound is a competitive antagonist of leukotriene D4 and E4. It can be used to study the role of leukotrienes in human asthma.
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| ln Vivo |
SR2640, with an IC50 of 3 nM, reduces the ileal contraction caused by LTD 4 in guinea pigs in a concentration-dependent manner [1]. The ileum and trachea of guinea pigs are selectively protected against contractile responses to LTD4 and LTE4 by SR2640 (1 mg/kg; i.v.; single dosage) [1].
In vivo, SR 2640 hydrochloride can be used to study the role of leukotrienes in human asthma. As a leukotriene receptor antagonist, it may modulate inflammatory responses in asthma and other conditions. However, detailed in vivo efficacy data for specific disease models are limited. SR 2640 hydrochloride is primarily used as a research tool for studying leukotriene biology. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for SR 2640 hydrochloride typically involve measuring its binding to leukotriene D4 and E4 receptors. The compound is a potent and selective competitive antagonist of these receptors. Radioligand binding assays using membrane preparations expressing these receptors are performed to determine the affinity. These assays confirm its mechanism of action as a leukotriene receptor antagonist.
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| Cell Assay |
In vitro cellular assays for SR 2640 hydrochloride typically involve measuring its ability to inhibit leukotriene-induced contraction of guinea pig ileum and trachea. The compound inhibits LTD4- but not histamine-induced contraction, with a pA2 of 8.7. These cell-based studies demonstrate its functional antagonism at leukotriene receptors and its selectivity over histamine receptors.
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| Animal Protocol |
Animal/Disease Models: guinea pig (injection of LTD4 and LTE4) [1]
Doses: 1 mg/kg Route of Administration: intravenous (iv) (iv)injection; single dose Experimental Results: specifically prevents the contractile response of guinea pig ileum and trachea to LTD4 and LTE4. In vivo animal models for SR 2640 hydrochloride may include models of asthma or inflammation to evaluate its efficacy as a leukotriene receptor antagonist. The compound is administered by appropriate routes, and inflammatory responses are assessed. However, detailed animal protocol information is limited. SR 2640 hydrochloride is primarily used as a research tool for studying leukotriene biology. |
| ADME/Pharmacokinetics |
SR 2640 hydrochloride has a molecular formula of C23H19ClN2O3 and a molecular weight of 406.86. Its CAS number is 146662-42-2. The compound is also known as SR2640 hydrochloride. It is a potent and selective competitive leukotriene D4 and E4 receptor antagonist. SR 2640 hydrochloride can be used to study the role of leukotrienes in human asthma.
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| Toxicity/Toxicokinetics |
SR 2640 hydrochloride is a leukotriene receptor antagonist with a well-characterized mechanism of action. As with any receptor antagonist, potential toxicity may include effects on inflammatory responses and immune function. The compound's safety profile should be evaluated in preclinical toxicology studies. SR 2640 hydrochloride is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying leukotriene biology and asthma.
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| References | |
| Additional Infomation |
SR 2640 hydrochloride (CAS# 146662-42-2) is a potent, selective, and competitive leukotriene D4 and E4 receptor antagonist. It inhibits LTD4- but not histamine-induced guinea pig ileum and trachea contraction with a pA2 of 8.7. SR 2640 hydrochloride can be used to study the role of leukotrienes in human asthma. The compound is for research use only and not for human therapeutic use.
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| Molecular Formula |
C23H18N2O3
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|---|---|
| Molecular Weight |
370.400625705719
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| Exact Mass |
406.108
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| CAS # |
146662-42-2
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| Related CAS # |
146662-42-2(HCl);105350-26-3;
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| PubChem CID |
45073453
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
514
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C=CC(=N2)COC3=CC=CC(=C3)NC4=CC=CC=C4C(=O)O.Cl
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| InChi Key |
KDSYWFCTUKABKE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H18N2O3.ClH/c26-23(27)20-9-2-4-11-22(20)24-17-7-5-8-19(14-17)28-15-18-13-12-16-6-1-3-10-21(16)25-18;/h1-14,24H,15H2,(H,26,27);1H
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| Chemical Name |
2-[3-(quinolin-2-ylmethoxy)anilino]benzoic acid;hydrochloride
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~250 mg/mL (~614.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.11 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 20.8 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: ≥ 2.08 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6998 mL | 13.4989 mL | 26.9978 mL | |
| 5 mM | 0.5400 mL | 2.6998 mL | 5.3996 mL | |
| 10 mM | 0.2700 mL | 1.3499 mL | 2.6998 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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