Date published: 2025-9-5

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CysLT1 Receptor Activators

CysLT1 activators are a group of chemicals that, while not directly binding and activating the CysLT1 receptor, play crucial roles in modulating the receptor's activity through various indirect mechanisms. These chemicals primarily influence the leukotriene pathway, which is intimately linked with the function of CysLT1 receptors. Leukotrienes are lipid mediators found in arachidonic acid, and their production and activity are central to the activation of CysLT1 receptors. Compounds like arachidonic acid and its metabolites, including leukotriene A4 and 5-HETE, are fundamental to the biosynthesis of leukotrienes. These substrates and intermediates, through enzymatic reactions, lead to the production of leukotriene C4, a potent activator of the CysLT1 receptor. Additionally, other chemicals, such as U46619, a thromboxane analogue, and prostaglandin E2, contribute to this pathway by modulating the production or action of leukotrienes. In contrast, some compounds, like aspirin, celecoxib, and MK-886, exert their influence on the CysLT1 receptor by altering the balance of different metabolic pathways within the arachidonic acid cascade. For instance, cyclooxygenase inhibitors can shift metabolism towards the lipoxygenase pathway, increasing leukotriene production. Moreover, certain leukotriene pathway inhibitors, like zileuton and nordihydroguaiaretic acid, can cause compensatory changes that eventually affect CysLT1 receptor activity. Montelukast, known as a CysLT1 antagonist, can also play a role in receptor regulation under specific conditions.

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Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Zafirlukast

107753-78-6sc-204942
sc-204942A
10 mg
100 mg
$36.00
$171.00
1
(1)

Zafirlukast functions as a potent antagonist of the cysteinyl leukotriene receptor 1 (CysLT1), exhibiting unique molecular interactions that disrupt leukotriene signaling pathways. Its structure facilitates specific binding to the receptor, altering conformational dynamics and inhibiting downstream inflammatory responses. The compound's kinetic profile reveals a competitive inhibition mechanism, characterized by a notable affinity for the receptor, which influences its interaction with various cellular environments.

Arachidonic Acid (20:4, n-6)

506-32-1sc-200770
sc-200770A
sc-200770B
100 mg
1 g
25 g
$90.00
$235.00
$4243.00
9
(1)

Arachidonic acid is a precursor in the leukotriene synthesis pathway. Its metabolism by 5-lipoxygenase leads to the production of leukotrienes, which can activate CysLT1 receptors.

5(S),6(R)-DiHETE

82948-88-7sc-200421
sc-200421A
50 µg
1 mg
$202.00
$2400.00
(0)

5(S),6(R)-DiHETE acts as an activator of the cysteinyl leukotriene receptor 1 (CysLT1), engaging in distinct molecular interactions that enhance receptor signaling. Its stereochemistry allows for precise binding, promoting conformational changes that trigger specific intracellular pathways. The compound exhibits unique reaction kinetics, facilitating rapid receptor activation and influencing downstream cellular responses, thereby modulating various physiological processes.

Leukotriene E4

75715-89-8sc-201050
sc-201050A
sc-201050B
sc-201050C
50 µg
1 mg
5 mg
10 mg
$207.00
$3570.00
$16320.00
$30600.00
(0)

Leukotriene A4, an intermediate in leukotriene biosynthesis, is converted into leukotriene C4, a known agonist of the CysLT1 receptor. This conversion indirectly enhances CysLT1 activation.

(±)5-HETE

73307-52-5sc-205136
sc-205136A
sc-205136B
25 µg
50 µg
100 µg
$89.00
$168.00
$319.00
1
(0)

5-HETE, a metabolite of arachidonic acid, serves as a substrate for leukotriene synthesis. Its availability can indirectly increase the activation of CysLT1 by facilitating the production of leukotriene C4.

U-46619

56985-40-1sc-201242
sc-201242A
1 mg
10 mg
$240.00
$1275.00
40
(4)

U46619, a thromboxane A2 analogue, can enhance the leukotriene pathway, indirectly leading to increased CysLT1 receptor activation.

A23187

52665-69-7sc-3591
sc-3591B
sc-3591A
sc-3591C
1 mg
5 mg
10 mg
25 mg
$54.00
$128.00
$199.00
$311.00
23
(1)

This compound increases intracellular calcium levels, which can enhance the activity of 5-lipoxygenase, leading to increased production of leukotrienes and indirect activation of CysLT1 receptors.

PGE2

363-24-6sc-201225
sc-201225C
sc-201225A
sc-201225B
1 mg
5 mg
10 mg
50 mg
$56.00
$156.00
$270.00
$665.00
37
(1)

Prostaglandin E2 can upregulate the leukotriene pathway, indirectly influencing CysLT1 receptor activation.

Aspirin

50-78-2sc-202471
sc-202471A
5 g
50 g
$20.00
$41.00
4
(1)

Aspirin can modulate the arachidonic acid pathway, leading to shifts in leukotriene production and indirect activation of CysLT1 receptors.

MK-886 sodium salt

118427-55-7sc-200608B
sc-200608
sc-200608A
1 mg
5 mg
25 mg
$46.00
$93.00
$371.00
3
(1)

MK-886 inhibits 5-lipoxygenase-activating protein (FLAP), indirectly influencing leukotriene synthesis and CysLT1 receptor activation.