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Protease Activated Receptor (PAR)

Protease-Activated Receptors (PARs) are a class of G protein-coupled receptors primarily activated by binding to and being cleaved by proteases. The PAR family includes PAR1, PAR2, PAR3, and PAR4, among which PAR1, PAR3, and PAR4 are primarily activated by thrombin, while PAR2 is primarily activated by trypsin and other proteases. PARs are involved in blood coagulation, vasoconstriction, and inflammatory responses. Abnormal activation of PARs is closely associated with thrombosis, cardiovascular diseases, and tumour metastasis.

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA
TP4040
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA is a bioactive peptide acting as a selective agonist for the protease-activated receptor 1 (PAR-1), demonstrating higher specificity for PAR-1 compared to PAR-2. PAR-1, part of the G protein-coupled receptor subfamily, is known to mediate cellular functions of thrombin. Beyond thrombin's various cellular roles, PAR-1 has been shown to interact with PAR-4, influencing thrombin-induced hepatocellular carcinoma, which forms thrombin in the tumor environment and is classified as "coagulation type."
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P2L-003
T2142851359416-20-8
P2L-003 is a selective PAR2 antagonist with an IC50 of 0.62 μM in HT-29 cells. It blocks PAR2-mediated Ca2+ mobilization without affecting signaling through PAR1, PAR4, or ATP. P2L-003 dose-dependently inhibits downstream MAPK signaling cascades, including the phosphorylation of ERK1/2 and p38, and is applicable in colon cancer research.
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10-14 weeks
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PAR2 modulator-1
T2145682378159-28-3
PAR2modulator-1 (Compound C781) is an antagonist of the protease-activated receptor 2 (PAR2). It specifically inhibits the PAR2-dependent MAPK signaling pathway with an IC50 value of 8.5 μM. PAR2modulator-1 can effectively block pain responses triggered by PAR2 agonists. This compound is useful for research in inflammation, immunology, and neurological disorders, including chronic pain and asthma.
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10-14 weeks
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