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Pranlukast (CAS 103177-37-3) LS-H18

CysLT1 receptor antagonist
LS-H18-10 / 10 mg / $175
LS-H18-100 / 100 mg / $235
LS-H18-500 / 500 mg / $515
LS-H18-1000 / 1000 mg / $875
USA Shipment Only
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Description: The cysteinyl leukotrienes (CysLT) LTC4 and LTD4 are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of G protein-coupled receptors, CysLT1 and CysLT2. Pranlukast (ONO-1078) is a potent, selective and orally active cysteinyl leukotriene1 (CysLT1) receptor antagonist. Sold under the trade name Ultair, it was the first cysteinyl (peptidyl) leukotriene receptor antagonist (LTRA) marketed for the treatment of asthma. Clinical studies in Japan, Europe, and North America all show that pranlukast significantly attenuates bronchoconstriction in response to a variety of allergen challenges as well as to inhaled LTD4. Pranlukast binds to the human CysLT1 and CysLT2 receptors with IC50 values of approximately 4-7 nM and 3,600 nM, respectively.

 

<div class="clearfi
H18_ChemicalStructureImage.png
N-[4-oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-benzamide
ONO-1078
Ultair
biochemical, chemical, antagonist
LS-H18
103177-37-3
C27H23N5O4
≥98%
A crystalline solid
 
O=C(Nc1cccc2c(=O)cc(oc12)c1[nH]nnn1)c1ccc(OCCCCc2ccccc2)cc1
InChI=1S/C27H23N5O4/c33-23-17-24(26-29-31-32-30-26)36-25-21(23)10-6-11-22(25)28-27(34)19-12-14-20(15-13-19)35-16-5-4-9-18-7-2-1-3-8-18/h1-3,6-8,10-15,17H,4-5,9,16H2,(H,28,34)(H,29,30,31,32)
NBQKINXMPLXUET-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: CYSLTR1 / CYSLT1 related products

Usage Information

Pranlukast is supplied as a crystalline solid. A stock solution may be made by dissolving the pranlukast in an organic solvent purged with an inert gas. Pranlukast is soluble in organic solvents such as DMSO and dimethyl formamide (DMF). The solubility of pranlukast in these solvents is approximately 10 and 20 mg/ml, respectively. Pranlukast is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, pranlukast should first be dissolved in DMF and then diluted with the aqueous buffer of choice. Pranlukast has a solubility of approximately 5 mg/ml in a 1:8 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Lynch, K.R., O’Neill, G.P., Liu, Q., et al. Nature 399, 789-793 (1999).
  2. Heise, C.E., O’Dowd, B.F., Figueroa, D.J., et al. J. Biol. Chem. 275, 30531-30536 (2000).
  3. Sarau, H.M., Ames, R.S., Chambers, J., et al. Mol. Pharmacol. 56, 657-663 (1999).
  4. Taniguchi, Y., Tamura, G., Honma, M., et al. J. Allergy Clin. Immunol. 92, 507-512 (1993).
  5. Barnes, N.C., de Jong, B., and Miyamoto, T. Chest 111, 52-60 (1997).

 


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