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HAMI3379 (CAS 712313-35-4) LS-H70

CysLT2 receptor antagonist
LS-H70-1 / 1 mg / $195
LS-H70-5 / 5 mg / $295
LS-H70-10 / 10 mg / $405
LS-H70-25 / 25 mg / $785
USA Shipment Only
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Description: The cysteinyl leukotrienes (CysLTs) 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. HAMI3379 is a potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 37.9 and >30,000 nM, respectively. In a CysLT2 receptor reporter cell line, HAMI3379 antagonizes LTD4- and LTC4-induced intracellular calcium mobilization with IC50 values of 3.8 and 4.4 nM, respectively, whereas it only weakly inhibits that for a CysLT1 receptor reporter cell line (IC50 = >10,000 nM). In isolated Langendorff-perfused guinea pig hearts, HAMI3379 reverses the LTC4-stimulated increase in perfusion pressure and decrease in contractility. H70_ChemicalStructureImage.png
3-[[(3-carboxycyclohexyl)amino]carbonyl]-4-[3-[4-[4-(cyclohexyloxy)butoxy]phenyl]propoxy]-benzoic acid
 
biochemical, chemical, antagonist
LS-H70
712313-35-4
C34H45NO8
≥90%
A crystalline solid
0
O=C(NC1CCCC(C(O)=O)C1)C2=CC(C(O)=O)=CC=C2OCCCC(C=C3)=CC=C3OCCCCOC4CCCCC4
InChI=1S/C34H39NO8/c36-32(35-27-10-6-9-25(22-27)33(37)38)30-23-26(34(39)40)15-18-31(30)43-21-7-8-24-13-16-29(17-14-24)42-20-5-4-19-41-28-11-2-1-3-12-28/h1-3,11-18,23,25,27H,4-10,19-22H2,(H,35,36)(H,37,38)(H,39,40)
GKPAULTWHHPIHX-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: CYSLT2 / CYSLTR2 related products

Usage Information

HAMI3379 is supplied as a crystalline solid. A stock solution may be made by dissolving the HAMI3379 in the solvent of choice. HAMI3379 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of HAMI3379 in ethanol is approximately 5 mg/ml and approximately 20 mg/ml in DMSO and DMF. HAMI3379 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, HAMI3379 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. HAMI3379 has a solubility of approximately 0.5 mg/ml in a 1:1 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. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399, 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, 30531-30536 (2000).
  3. Sarau, H.M., Ames, R.S., Chambers, J., et al. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Mol. Pharmacol. 56, 657-663 (1999).
  4. Wunder, F., Tinel, H., Kast, R., et al. Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT2) receptor. Br. J. Pharmacol. 160, 399-409 (2010).

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