HAMI3379 - CAS 712313-35-4
Catalog number:
712313-35-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C34H45NO8
Molecular Weight:
595.73
COA:
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Targets:
Leukotriene Receptor
Description:
HAMI3379 is a cysteinyl leukotriene 2 (CysLT2) receptor antagonist. It can inhibit radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 37.9 and >30,000 nM. In a CysLT2 receptor reporter cell line, it can antagonize LTD4- and LTC4-induced intracellular calcium mobilization with IC50 values of 3.8 and 4.4 nM, respectively, but it only weakly inhibits that for a CysLT1 receptor reporter cell line with IC50 value >10,000 nM. HAMI3379 may represent a new type of therapeutic agent in the treatment of ischemic stroke.
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Purity:
90%
Appearance:
A crystalline solid
Synonyms:
CHEMBL3342944;GTPL6197; SCHEMBL4518791; DTXSID80439859;3-[(3-carboxycyclohexyl)carbamoyl]-4-[3-[4-(4-cyclohexyloxybutoxy)phenyl]propoxy]benzoic acid
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
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Application:
ischemic stroke
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
HRJWSEPIRZRGCL-UHFFFAOYSA-N
InChI:
InChI=1S/C34H45NO8/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/h13-18,23,25,27-28H,1-12,19-22H2,(H,35,36)(H,37,38)(H,39,40)
Canonical SMILES:
C1CCC(CC1)OCCCCOC2=CC=C(C=C2)CCCOC3=C(C=C(C=C3)C(=O)O)C(=O)NC4CCCC(C4)C(=O)O
1.[Antioxidative effects of cysteinyl leukotriene receptor antagonists montelukast and HAMI 3379 on ischemic injury in rat cortical neurons in vitro].
Xu DM1, Zhang XY1, Wang XR1, Chen L2, Zhang LH3, Shi QJ1, Fang SH1, Lu YB1, Zhang WP1, Wei EQ1. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2014 May;43(3):257-64.
OBJECTIVE: To investigate the antioxidative effects of two cysteinyl leukotriene receptors antagonists (CysLT1R and CysLT2R) montelukast and HAMI 3379 on ischemic injury of rat cortical neurons in vitro.
2.Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.
Wunder F1, Tinel H, Kast R, Geerts A, Becker EM, Kolkhof P, Hütter J, Ergüden J, Härter M. Br J Pharmacol. 2010 May;160(2):399-409. doi: 10.1111/j.1476-5381.2010.00730.x.
BACKGROUND AND PURPOSE: Cysteinyl leukotrienes (CysLTs) have been implicated in the pathophysiology of inflammatory and cardiovascular disorders. Their actions are mediated by CysLT(1) and CysLT(2) receptors. Here we report the discovery of 3-({[(1S,3S)-3-carboxycyclohexyl]amino}carbonyl)-4-(3-{4-[4-(cyclo-hexyloxy)butoxy]phenyl}propoxy) benzoic acid (HAMI3379), the first potent and selective CysLT(2) receptor antagonist.
3.Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists.
Dong X1, Zhao Y, Huang X, Lin K, Chen J, Wei E, Liu T, Hu Y. Eur J Med Chem. 2013 Apr;62:754-63. doi: 10.1016/j.ejmech.2013.01.041. Epub 2013 Feb 9.
3D structure of CysLT2 receptor was constructed by using homology modeling and molecular simulations. The binding pocket of CysLT2 receptor and the proposition of the interaction mode between CysLT2 and HAMI3379 were identified. A series of dicarboxylated chalcones was then virtually evaluated through molecular docking studies. A total of six compounds 13a-f with preferable scores was further synthesized and tested for CysLT2 antagonistic activities by determination of the cytosolic free Ca(2+) levels in HEK293 cells. Compounds 13e and 13f exhibited potent and selective CysLT2 antagonistic activities with IC50 values being 7.5 and 0.25 μM, respectively.
4.ERK/Egr-1 signaling pathway is involved in CysLT2 receptor-mediated IL-8 production in HEK293 cells.
Lin K1, Fang S2, Cai B1, Huang X3, Zhang X3, Lu Y3, Zhang W3, Wei E3. Eur J Cell Biol. 2014 Jul;93(7):278-88. doi: 10.1016/j.ejcb.2014.05.001. Epub 2014 May 20.
The CysLT2 receptor is involved in myocardial ischemia/reperfusion injury, differentiation of colorectal cancers, bleomycin-induced pulmonary inflammation and fibrosis. However, the signal transduction of cysteinyl leukotriene receptor 2 (CysLT2) in inflammatory responses remains to be clarified. In HEK293 cells stably expressing hCysLT1, hCysLT2 and rGPR17, we determined the signaling pathways for interleukin-8 (IL-8) production after CysLT2 receptor activation. HEK293 cells were stably transfected with the recombinant plasmids of pcDNA3.1(+)-hCysLT1, pcDNA3.1(+)-hCysLT2 and pcDNA3.1-rGPR17. Leukotriene C4 (LTC4) and LTD4 were used as the agonists to induce IL-8 production and the related changes in signal molecules. We found that LTC4 and LTD4 significantly induced IL-8 promoter activation in the HEK293 cells stably expressing hCysLT2, but not in those expressing hCysLT1 and rGPR17. In hCysLT2-HEK293 cells, LTC4 induced elevation of intracellular calcium, ERK1/2 phosphorylation and Egr-1 expression, and stimulated IL-8 expression and release.
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CAS 712313-35-4 HAMI3379

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