1. GPCR/G Protein
  2. Leukotriene Receptor
  3. HAMI 3379

HAMI 3379 

Cat. No.: HY-112248 Purity: >95.0%
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HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT2) receptor antagonist. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury, and attenuates microglia-related inflammation.

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HAMI 3379 Chemical Structure

HAMI 3379 Chemical Structure

CAS No. : 712313-35-4

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Description

HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT2) receptor antagonist[1]. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury, and attenuates microglia-related inflammation[2].

IC50 & Target[1]

CysLT2

 

In Vitro

In a CysLT2 receptor reporter cell line, HAMI 3379 antagonizes leukotriene D4- (LTD4-) and leukotriene C4- (LTC4-) induced intracellular calcium mobilization with IC50 values of 3.8 nM and 4.4 nM, respectively. In contrast, HAMI 3379 exhibits very low potency on a recombinant CysLT1 receptor cell line (IC50>10000 nM)[1].

In Vivo

HAMI 3379 (ip; 0.025-0.4 mg/kg; 24 hours) attenuates the acute brain injury 24 hours after middle cerebral artery occlusion (MCAO) with effective doses of 0.1-0.4 mg/kg and a therapeutic window of ∼1 hour. It attenuates the neurological deficits, and reduces infarct volume, brain edema, and neuronal loss and degeneration 24 and 72 hours after MCAO[2].
HAMI 3379 (infused into the aortic cannula at a rate of 1% of the total flow rate; 0.01, 0.1, 1 μM; 20 min) concentration-dependently inhibits and reverses the LTC4-induced perfusion pressure increase and contractility decrease[1].

Animal Model: Male Sprague-Dawley rats (250-300 g) after MCAO[2]
Dosage: 0.025, 0.05, 0.1, 0.2, 0.4 mg/kg
Administration: IP; 24 hours
Result: Attenuated the acute brain injury 24 hours after MCAO with effective doses of 0.1-0.4 mg/kg and a therapeutic window of ∼1 hour.
Molecular Weight

595.72

Formula

C₃₄H₄₅NO₈

CAS No.

712313-35-4

SMILES

O=C(O)C1=CC=C(OCCCC2=CC=C(OCCCCOC3CCCCC3)C=C2)C(C(NC4CC(C(O)=O)CCC4)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >95.0%

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Keywords:

HAMI 3379HAMI3379HAMI-3379Leukotriene ReceptorCysteinylleukotrieneCysLT2CysLTprotectivebraininjurymicroglia-relatedinflammationInhibitorinhibitorinhibit

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HAMI 3379
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HY-112248
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