For research use only. Not for therapeutic Use.
HAMI 3379 is a potent and selective CysLT2 receptor antagonist. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury, and attenuates microglia-related inflammation[1][2].
In a CysLT2 receptor reporter cell line, HAMI3379 antagonizes leukotriene D4- (LTD4-) and leukotriene C4- (LTC4-) induced intracellular calcium mobilization with IC50 values of 3.8 nM and 4.4 nM respectively. HAMI3379 exhibits very low potency on a recombinant CysLT1 receptor cell line (IC50>10000 nM). HAMI3379 does not exhibit any agonistic activity on both CysLT receptor cell lines[1].
HAMI 3379 (0.025-0.4 mg/kg; ip) with 0.1-0.4 mg/kg significantly reduces the infarct volume and percentage increase in the ischemic/contralateral hemispheric ratio[2].
HAMI3379 (0.1 mg/kg; ip) administered at 0 and 1 h after reperfusion reduces infarct volume, attenuated brain edema, reduced neurological score, and increased holdingangle[2].
Catalog Number | I045614 |
CAS Number | 1245653-57-9 |
Synonyms | 3-[[(1S,3S)-3-carboxycyclohexyl]carbamoyl]-4-[3-[4-(4-cyclohexyloxybutoxy)phenyl]propoxy]benzoic acid |
Molecular Formula | C34H45NO8 |
Purity | ≥95% |
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)/t25-,27-/m0/s1 |
InChIKey | HRJWSEPIRZRGCL-BDYUSTAISA-N |
SMILES | C1CCC(CC1)OCCCCOC2=CC=C(C=C2)CCCOC3=C(C=C(C=C3)C(=O)O)C(=O)NC4CCCC(C4)C(=O)O |
Reference | [1]. F Wunder, et al. Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor. Br J Pharmacol. 2010 May;160(2):399-409. [2]. Q J Shi, et al. HAMI 3379, a CysLT2R antagonist, dose- and time-dependently attenuates brain injury and inhibits microglial inflammation after focal cerebral ischemia in rats. Neuroscience. 2015 Apr 16;291:53-69. |