| Bioactivity | 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]. | |||||||||
| Invitro | 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]. | |||||||||
| In Vivo | 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]. Animal Model: | |||||||||
| Name | HAMI 3379 | |||||||||
| CAS | 1245653-57-9 | |||||||||
| Formula | C34H45NO8 | |||||||||
| Molar Mass | 595.72 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| 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. |