cyslt2

Gemilukast (ONO-6950) is an orally active and potent dual inhibitor of cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2), inhibits LTC 4-induced bronchoconstriction, and is inhibitory to human CysLT1 and CysLT2, and may be used in the treatment of asthma.

HAMI 3379 is a potent and selective antagonist of the Cysteinyl leukotriene (CysLT2) receptor. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury. It also attenuates microglia-related inflammation.

ONO 2050297 (Compound 19) is a selective cysteinyl leukotriene (CysLT) antagonist, with IC50 values of 17 nM for CysLT1 and 0.87 nM for CysLT2. It is applicable for research in bronchial asthma.

Quininib is a selective antagonist of CysLTR1 and CysLTR2, with IC50 values of 1.2 and 52 μM, respectively, exhibiting anti-angiogenic and anti-tumour effects.

BAY-u 9773 is a non-selective antagonist of cysteinyl leukotrienes receptors (CysLT receptors), with approximately equal IC50 values for both CysLT1 and CysLT2. BAY-u 9773 is used to inhibit leukotriene responses [1].

N-methyl Leukotriene C4 (250 μg/ml solution in ethanol) is a metabolically stable synthetic analogue of Leukotriene C4 that resists enzymatic conversion into LTD4 and LTE4. N-methyl Leukotriene C4 is a valuable experimental tool for investigations involving leukotriene signaling, inflammatory mediator biology, eicosanoid metabolism, and receptor-associated inflammatory pathways.

HAMI 3379 (HAMI3379) is a selective cysteinyl leukotriene receptor 2 (CysLT2) antagonist that dose- and time-dependently attenuates brain damage and inhibits microglial cell inflammation following focal cerebral ischemia in rats and attenuates ischemia-like neuronal damage by inhibiting microglial activation.

ONO-4310321 is a potent, orally available dual CysLT1 and CysLT2 receptor antagonist.

ONO-2050297 is the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.

S-Geranylgeranyl-L-glutathione acts as a ligand for the orphan G protein-coupled receptor (GPCR) P2RY8, displaying selective affinity by inducing internalization of P2RY8 in preference to the sphingosine-1-phosphate receptor 2 (S1P2), GPR55, cysteinyl leukotriene receptor 1 (CysLT1 receptor), and the CysLT2 receptor at a concentration of 100 nM. Additionally, at a lower concentration of 10 nM, S-Geranylgeranyl-L-glutathione inhibits the chemokine (C-X-C motif) ligand 12-induced migration of both P2RY8-expressing WEHI-231 B cell lymphoma cells and human tonsil germinal center B cells.