>>Signaling Pathways>> Proteases>> Lipoxygenase>>Pranlukast-d4

Pranlukast-d4 (Synonyms: ONO-1078-d4)

Catalog No.GC45768

A neuropeptide with diverse biological activities

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Pranlukast-d4 Chemical Structure

Cas No.: 2713172-43-9

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1mg
US$556.00
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Sample solution is provided at 25 µL, 10mM.

Description of Pranlukast-d4

Pranlukast-d4 is intended for use as an internal standard for the quantification of pranlukast by GC- or LC-MS. Pranlukast is an orally bioavailable cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50s = 4.3-7.2 nM in radioligand binding assays).1 It is selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3,620 nM for the human receptor).2 Pranlukast inhibits mucus secretion induced by leukotriene D4 in isolated guinea pig trachea with an IC50 value of 0.3 μM.3 It inhibits TNF-α-induced NF-•B p65 nuclear localization in U937 and Jurkat cells when used at concentrations of 10 and 100 μM.4 Pranlukast inhibits bronchoconstriction induced by LTC4 , LTD4, and LTE4 , but not LTB4 , in guinea pigs (ID50s = 0.8, 1, 0.7, and >500 μg/kg, respectively).5 It reduces cortical infarct volume by 81.6% and decreases neuronal death in the cortex, hippocampus, and striatum in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 0.03 mg/kg.6

|1. Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399(6738), 789-793 (1999).|2. Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J. Biol. Chem. 275(39), 30531-30536 (2000).|3. Liu, Y.-C., Khawaja, A.M., and Rogers, D.F. Effects of the cysteinyl leukotriene receptor antagonists pranlukast and zafirlukast on tracheal mucus secretion in ovalbumin-sensitized guinea-pigs in vitro. Br. J. Pharmacol. 124(3), 563-571 (1998).|4. Ichiyama, T., Hasegawa, S., Umeda, M., et al. Pranlukast inhibits NF-KB activation in human monocytes/macrophages and T cells. Clin. Exp. Allergy 33(6), 802-807 (2003).|5. Nakai, H., Konno, M., Kosuge, S., et al. New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships. J. Med. Chem. 31(1), 84-91 (1988).|6. Zhang, W.-P., Wei, E.-Q., Mei, R.-H., et al. Neuroprotective effect of ONO-1078, a leukotriene receptor antagonist, on focal cerebral ischemia in rats. Acta Pharmacol. Sin. 23(10), 871-877 (2002).

Chemical Properties of Pranlukast-d4

Cas No. 2713172-43-9 SDF
Synonyms ONO-1078-d4
Canonical SMILES O=C1C=C(C2=NN=NN2)OC(C1=CC=C3)=C3NC(C4=C([2H])C([2H])=C(C([2H])=C4[2H])OCCCCC5=CC=CC=C5)=O
Formula C27H19D4N5O4 M.Wt 485.5
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Pranlukast-d4

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1 mg 5 mg 10 mg
1 mM 2.0597 mL 10.2987 mL 20.5973 mL
5 mM 0.4119 mL 2.0597 mL 4.1195 mL
10 mM 0.206 mL 1.0299 mL 2.0597 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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