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SR 2640 hydrochloride

Potent, selective LTD4 /LTE4 receptor antagonist CAS# 146662-42-2

SR 2640 hydrochloride

2D Structure

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SR 2640 hydrochloride

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Chemical Properties of SR 2640 hydrochloride

Cas No. 146662-42-2 SDF Download SDF
PubChem ID 45073453 Appearance Powder
Formula C23H19ClN2O3 M.Wt 406.87
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name 2-[3-(quinolin-2-ylmethoxy)anilino]benzoic acid;hydrochloride
SMILES C1=CC=C2C(=C1)C=CC(=N2)COC3=CC=CC(=C3)NC4=CC=CC=C4C(=O)O.Cl
Standard InChIKey KDSYWFCTUKABKE-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

SR 2640 hydrochloride Dilution Calculator

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SR 2640 hydrochloride Molarity Calculator

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Preparing Stock Solutions of SR 2640 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4578 mL 12.2889 mL 24.5779 mL 49.1557 mL 61.4447 mL
5 mM 0.4916 mL 2.4578 mL 4.9156 mL 9.8311 mL 12.2889 mL
10 mM 0.2458 mL 1.2289 mL 2.4578 mL 4.9156 mL 6.1445 mL
50 mM 0.0492 mL 0.2458 mL 0.4916 mL 0.9831 mL 1.2289 mL
100 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.4916 mL 0.6144 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SR 2640 hydrochloride

LTD4 increases cytosolic free calcium and inositol phosphates in human neutrophils: inhibition by the novel LTD4 receptor antagonist, SR2640, and possible relation to modulation of chemotaxis.[Pubmed:2160189]

Agents Actions. 1990 Mar;29(3-4):299-307.

LTD4 increased the level of free intracellular calcium ([Ca++]i) and stimulated the production of inositol phosphates (IP) in human polymorphonuclear neutrophils (PMN). Calcium was predominantly mobilized from intracellular pools. After a single stimulus, the cells were refractory to a second challenge with the same concentration of LTD4, but the calcium response to LTB4 was normal. The rise in [Ca++]i as well as the stimulated production of IP was inhibited by the novel LTD4 antagonist, SR2640. SR2640 also abolished the attenuation by LTD4 of LTB4-directed PMN chemotaxis. The results suggest that human PMN contain specific LTD4 receptor that trigger phosphatidyl inositol hydrolysis by activation of phospholipase C, leading to intracellular calcium mobilization, which may be involved in modulation of chemotaxis.

Inhibition by the LTD4 antagonist, SR2640, of effects of LTD4 on canine polymorphonuclear leukocyte functions.[Pubmed:2546563]

Biochem Pharmacol. 1989 Jul 15;38(14):2291-5.

The sulfidopeptide leukotriene LTD4 selectively inhibited directed migration of canine polymorphonuclear leukocytes towards LTB4 (100 nM) with an IC50 of 38 nM. No effect on PAF-acether induced migration was observed. LTD4 did not cause detectable adherence of cells to the Boyden chamber system. Neither LTD4 nor the LTD4/LTE4 receptor antagonist, SR2640, possessed chemokinetic properties. LTD4 induced reversible aggregation of the cells with an EC50 of 36 nM. SR2640 suppressed or abolished LTD4 responses in vitro and following oral administration of the drug. SR2640 had no effect on aggregation induced by LTB4 or PAF-acether. The results can be taken as evidence that canine polymorphonuclear leukocytes possess LTD4 receptors that may be involved in a leukotriene specific micro-feedback system between the different cell types involved in inflammatory responses.

A novel leukotriene D4/E4 antagonist, SR2640 (2-[3-(2-quinolylmethoxy)phenylamino]benzoic acid).[Pubmed:2854067]

Eur J Pharmacol. 1988 Oct 11;155(1-2):117-28.

We have studied the leukotriene antagonistic activity of a novel compound, SR2640 (2-[3-(2-quinolylmethoxy)phenylamino]benzoic acid), in vitro and in vivo. SR2640 inhibited LTD4- but not histamine-induced contractions of guinea-pig ileum and trachea in a concentration-dependent manner. Schild plot analysis of tracheal LTD4 antagonism yielded a pA2 value of 8.7 and a slope not different from unity. SR2640 concentration dependently inhibited the binding of 0.4 nM [3H]LTD4 to guinea-pig lung membranes with an IC50 value of 23 nM. The curve was parallel to that of unlabelled LTD4 (IC50 = 2.2 nM). SR2640 was equally effective in antagonizing LTD4 and LTE4, but was much less potent in reducing LTC4-induced ileum contractions. In vivo, SR2640 in the dose range 0.03-1.00 mg/kg shifted the dose-response curve for guinea-pig bronchoconstriction induced by intravenous LTD4 administration to the right at a rate proportional to the dose of SR2640, without reducing the maximum attainable obstruction: the slope of the Schild plot was 0.99. SR2640 (1 mg/kg) also caused a significant inhibition of antigen-induced bronchoconstriction in anaesthetized guinea-pigs pretreated with pyrilamine, indomethacin, propranolol and suxamethonium. In conclusion, SR2640 appears to be a potent and selective competitive LTD4/LTE4 antagonist, and may be useful in elucidating the role of leukotrienes in human asthma.

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