A CysLT2 receptor antagonist
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HAMI3379

Item No. 10580

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[[(1S,3S)-3-carboxycyclohexyl]amino]carbonyl]-4-[3-[4-[4-(cyclohexyloxy)butoxy]phenyl]propoxy]-benzoic acid
CAS Number
1245653-57-9
Molecular Formula
C34H45NO8
Formula Weight
595.7
Purity
≥90%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 5 mg/ml
λmax
220 nm
SMILES
O=C(N[C@H]1CCC[C@H](C(O)=O)C1)C2=CC(C(O)=O)=CC=C2OCCCC(C=C3)=CC=C3OCCCCOC4CCCCC4
InChi Code
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
InChi Key
HRJWSEPIRZRGCL-GPNIZQGCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $61

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    5 mg

    $260

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    10 mg

    $462

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    25 mg

    $1,006

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    Product Description

    HAMI3379 is a cysteinyl leukotriene 2 (CysLT2) receptor antagonist (IC50 = 37.9 nM in a radioligand binding assay).1 It is selective for CysLT2 over CysLT1 (IC50 = >30 µM in a radioligand binding assay). HAMI3379 inhibits calcium mobilization induced by leukotriene D4 (LTD4; Item No. 20310) or leukotriene C4 (LTC4; Item No. 20210) in CHO cells expressing human CysLT2 (IC50s = 3.8 and 4.4 nM, respectively). It reverses the LTC4-induced increases in perfusion pressure and decreases in contractility in isolated Langendorff-perfused guinea pig hearts in a concentration-dependent manner. HAMI3379 (0.1 mg/kg) prevents decreases in body weight and neurological deficit scores in a rat model of S. pneumoniae-induced meningitis, as well as reduces infarct volume in a rat model of cerebral ischemia brain injury induced by middle cerebral artery occlusion (MCAO).2,3 It also prevents increases in airway hyperresponsiveness in a mouse model of ovalbumin-induced asthma when administered at a dose of 10 mg/kg.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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(2), 399-409 (2010).

    2. Yu, S., Chen, X., Li, X., et al. Neuroprotective effects of CysLTR antagonist on Streptococcus pneumoniae‑induced meningitis in rats. Exp. Ther. Med. 24(1), 443 (2022).

    3. Shi, Q.J., Wang, H., Liu, Z.X., 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 291, 53-69 (2015).

    4. Trinh, H.K.T., Suh, D.-H., Nguyen, T.V.T., et al. Characterization of cysteinyl leukotriene-related receptors and their interactions in a mouse model of asthma. Prostaglandins Leukot. Essent. Fatty Acids 141, 17-23 (2019).

    Product Citations

    Yu, S., Chen, X., Li, X., et al. Neuroprotective effects of CysLTR antagonist on Streptococcus pneumoniae‑induced meningitis in rats. Exp. Ther. Med. 24(1), 443 (2022).