2. Signaling Pathways
  3. GPCR/G Protein
  4. Leukotriene Receptor

Leukotriene Receptor

Leukotriene Receptor

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Leukotriene Receptor (cys-LTs) are a family of potent bioactive lipids that act through two structurally divergent G protein-coupled receptors, termed the CysLT1 and CysLT2 receptors. The cysteinyl leukotrienes LTC4, LTD4, and LTE4 are important mediators of human bronchial asthma. Leukotriene Receptor is a member of the superfamily of G protein-coupled receptors and uses a phosphatidylinositol-calcium second messenger system. Activation of CysLT1 by LTD4 results in contraction and proliferation of smooth muscle, oedema, eosinophil migration and damage to the mucus layer in the lung. Leukotriene receptor antagonists, called LTRAs for short, are a class of oral medication that is non-steroidal. They may also be referred to as anti-inflammatory bronchoconstriction preventors. LTRAs work by blocking a chemical reaction that can lead to inflammation in the airways.

Leukotriene Receptor Isoform Specific Products:

Leukotriene Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-122536
    Ricinelaidic acid
    		Antagonist
    Ricinelaidic acid, a 12-hydroxy fatty acid，is a leukotriene B4 (LTB4) receptor antagonist with the Ki of 2 μM in porcine neutrophil membranes. Ricinelaidic acid inhibits chemotaxis and calcium flux induced by LTB4 in isolated human neutrophils (IC50=10 and 7 μM, respectively). Ricinelaidic acid inhibits bronchoconstriction induced by LTB4 in rats.
    Ricinelaidic acid
  • HY-19041
    CGP-35949 sodium
    		Antagonist
    CGP-35949 sodium is a LTD4 antagonist with phospholipase inhibitory activity. CGP-35949 sodium can be used for research of asthma.
    CGP-35949 sodium
  • HY-120755
    LY290324
    		Antagonist
    LY290324 is a potent and orally active leukotriene D4 (LTD4) antagonist. LY290324 reduces LTC4, LTD4 and LTE4 (HY-113465)-induced bronchospasm. LY290324 has the potential for the research of antigen-induced bronchospasm.
    LY290324
  • HY-17492S3
    Zafirlukast-d6
    		Antagonist
    Zafirlukast-d6 is deuterated labeled Zafirlukast (HY-17492). Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
    Zafirlukast-d<sub>6</sub>
  • HY-101438AR
    Darbufelone mesylate (Standard)
    		Inhibitor
    Darbufelone (mesylate) (Standard) is the analytical standard of Darbufelone (mesylate) (HY-101438A). This product is intended for research and analytical applications. Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
    Darbufelone mesylate (Standard)
  • HY-122175
    ZK-158252
    		Antagonist
    ZK-158252 is a leukotriene B4 type-2 receptor (BLT2) antagonist.
    ZK-158252
  • HY-125408
    Maresin conjugates in tissue regeneration 1
    		Antagonist
    Maresin conjugates in tissue regeneration 1 (MCTR1) is a potent cytokine of pro-resolving mediating maresin conjugates in tissue regeneration (MCTR), which reduces the inflammatory response and promotes tissue regeneration. Maresin conjugates in tissue regeneration 1 antagonize LTD4-stimulated vascular responses.
    Maresin conjugates in tissue regeneration 1
  • HY-122149
    L-648051
    		Antagonist
    L-648051 is a leukotriene D4 receptor (LTD4) antagonist. L-648051 plays an important role in arrhythmias.
    L-648051
  • HY-117706
    LY 292728
    		Antagonist
    LY 292728 is a potent leukotriene B4 (LTB4) receptor antagonist. LY 292728 binds to human neutrophils with a Ki of 0.47 nM and binds to guinea pig lung membranes with a Ki of 0.04 nM.
    LY 292728
  • HY-108396R
    γ-Linolenic acid ethyl ester (Standard)
    		Antagonist
    γ-Linolenic acid ethyl ester (Standard) is the analytical standard of γ-Linolenic acid ethyl ester (HY-108396). This product is intended for research and analytical applications. γ-Linolenic acid ethyl ester (Ethyl γ-linolenate) is a leukotriene B4 receptor 4 (LTB4) antagonist.
    γ-Linolenic acid ethyl ester (Standard)
  • HY-107608S1
    Leukotriene B4-d5
    Leukotriene B4-d5 (LTB4-d5) is deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
    Leukotriene B4-d<sub>5</sub>
  • HY-101676R
    RG-12525 (Standard)
    		Antagonist
    RG-12525 (Standard) is the analytical standard of RG-12525 (HY-101676). This product is intended for research and analytical applications. RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 μM.
    RG-12525 (Standard)
  • HY-117557
    LY306669
    		Antagonist
    LY306669 is a potent and selective leukotriene B4 (LTB4) receptor antagonist that can be used for the research of lung injury.
    LY306669
  • HY-13628R
    Etalocib (Standard)
    		Antagonist
    Etalocib (Standard) is the analytical standard of Etalocib. This product is intended for research and analytical applications. Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
    Etalocib (Standard)
  • HY-176921
    ONO-2570366
    		Antagonist
    ONO-2570366 (Compound 11a) is an antagonist of the cysteinyl leukotriene receptors CysLT1R and CysLT2R (IC50 = 14 nM). ONO-2570366 inhibits the binding of LTD4
    ONO-2570366
  • HY-118848
    A63162
    A63162 is a specific 5-lipoxygenase (5-LOX) inhibitor. A63162 inhibits mitogen (PHA)-induced horse mononuclear cell (BMC) proliferation and inhibits Calcimycin (HY-N6687)-induced leukotriene LTB4 synthesis at the same concentration. A63162 can be used in the study of chronic obstructive pulmonary disease, arthritis and inflammatory bowel disease.
    A63162
  • HY-N2056R
    11-Keto-beta-boswellic acid (Standard)
    		Inhibitor
    11-Keto-beta-boswellic acid (Standard) is the analytical standard of 11-?Keto-?beta-?boswellic acid. This product is intended for research and analytical applications. 11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.
    11-Keto-beta-boswellic acid (Standard)
  • HY-W612175
    H-Ala-pNA
    		Substrate
    H-Ala-pNA is an L-amino acid p-nitroaniline (pNA) derivative and a specific substrate for leukotriene A4 hydrolase. The D-enantiomer of H-Ala-pNA shows no activity toward leukotriene A4 hydrolase. H-Ala-pNA can be catalytically hydrolyzed by leukotriene A4 hydrolase, and the p-nitroaniline produced during the reaction is monitored spectrophotometrically at 405 nm to enable quantitative detection of enzyme activity. H-Ala-pNA is used to evaluate the potency of inhibitors targeting the amidase activity of leukotriene A4 hydrolase.
    H-Ala-pNA
  • HY-14166R
    MK-886 (Standard)
    		Inhibitor
    MK-886 (Standard) is the analytical standard of MK-886. This product is intended for research and analytical applications. MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.
    MK-886 (Standard)
  • HY-101731
    CP-96021 hydrochloride
    		Antagonist
    CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Ki values of 34 nM and 37 nM, respectively.
    CP-96021 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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