thrombin receptor activator peptide-6

Thrombin Receptor Activator for Peptide is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).

Epidermal Growth Factor Receptor Peptide Acetate (Epidermal Growth Factor Receptor Peptide Acetate(96249-43-3 Free base)) exists on the cell surface and is activated by the binding of its specific ligands.EGFR belongs to the ErbB family of receptor tyrosine kinases (RTK).

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is employed in coronary heart disease (CHD) research.

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β with a remarkable affinity (K i = 0.44 nM). This compound exhibits an impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor, and it produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

RXFP1 receptor agonist-6 (Example 7) serves as an agonist for the RXFP1 receptor and effectively suppresses cAMP production in HEK293 cells that stably express the human RXFP1, exhibiting an EC50 of 12 nM [1].

Compound Z10 (PKM2 activator 6) serves as both a PKM2 activator and a PDK1 inhibitor, exhibiting dissociation constants (K D ) of 121 μM and 19.6 μM, respectively. It promotes apoptosis in colorectal cells while suppressing their proliferation and migration, additionally inhibiting glycolysis. Compound Z10 demonstrates inhibitory effects on the proliferation of various cell lines, including DLD-1, HCT-8, HT-29, and MCF-10A, with half-maximal inhibitory concentrations (IC 50 ) of 10.04 μM, 2.16 μM, 3.57 μM, and 66.39 μM, as recorded in reference [1].

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

Thrombin Inhibitor 6, with an IC 50 of 1 nM, acts as a potent anticoagulant by inhibiting thrombin.

NMDA receptor regulator 6 (Compound 183) is an effective NMDA receptor regulator and has research value in neurological disorders.

GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with low cellular membrane permeability (Ki = 0.56 μM) [1].

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

NMDA Receptor Antagonist 6 (Compound 13b) functions as an antagonist at the glycine-binding site of the NMDA receptor and demonstrates cytoneuroprotective efficacy. It safeguards PC12 cells from NMDA-induced damage and apoptosis [1].

APJ receptor agonist 6 is a potent agonist of the APJ (apelin receptor) (Ki: 0.059 μM). (EC50: 6.22 μM).

Interleukin (IL)-6 Receptor is a peptide.

IFN-α Receptor Recognition Peptide 1, associated with receptor interactions, is a peptide of IFN-α.

The signal transducer and activator of transcription 6 fragments is a peptide with the sequence H2N-Ser-Tyr-Trp-Ser-Asp-Arg-Leu-Ile-Ile-OH, MW= 1152.3.

TFRGAP-amide, human PAR-3-derived tethered ligand sequence which does not activate PAR-3 but rather activates PAR-1 and PAR-2, either in Jurkat or in other PAR-expressing cells.

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a peptide that acts as an agonist for the proteinase-activated receptor (PAR-3)[1].

TRAP-6 peptide is a hexapeptide corresponding to residues 42-47 of protease-activated receptor 1 (PAR1). It acts as an agonist of PAR1, inducing platelet aggregation in human platelet-rich plasma ex vivo (EC50 = 0.8 μM). TRAP-6 (0.3 and 0.6 mg/kg) has a triphasic effect on mean arterial blood pressure (MAP) in anesthetized rats with a short decrease, an increase, and then a longer decrease in MAP following intravenous administration.

Thrombin receptor peptide ligand is antagonist of the thrombin receptor (EC50s = 16-33 μM to inhibit platelet aggregation in vitro). It inhibits α-thrombin and platelet aggregation induced by thrombin receptor activating peptide in vitro when used at a concentration of 32 μM but does not affect platelet aggregation induced by ADP or collagen. It also inhibits thrombin- and TRAP-induced proliferation of vascular smooth muscle cells (VSMCs). Thrombin receptor peptide ligand (100 μmol/kg bolus, i.v., plus 900 μmol/kg infusion) inhibits arterial thrombosis in a rabbit model of partial carotid artery occlusion without increasing bleeding time.

AMPK activator 6 (Compound GC) activates the AMPK pathway and reduces lipid content in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase of total cholesterol (TC), low-density lipoprotein-C (LDL-C), triglyceride (TG), and other biochemical indices in blood serum. AMPK activator 6 has research value in non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome .

AMPA receptor modulator-6, an AMPA receptor positive allosteric modulator (PAM), is utilized in the research of neurological diseases [1].

Thrombin receptor peptide ligand, a thrombin receptor antagonist, serves as an antithrombotic agent [1].

Nrf2 Activator-6, a tetrahydroisoquinoline compound, functions as an Nrf2 activator, demonstrating potency with an IC50 value of 5 nM in inhibiting the Kelch domain-Nrf2 interaction.

Casein Kinase II Receptor Peptide, a substrate for casein kinase II, exhibits a Km value of 500 µM. It is utilized to measure the activity of casein kinase II in crude enzyme preparations [1].

Estrogen receptor antagonist 6 is a potent antagonist of the Estrogen receptor. Estrogen receptor is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. Compound 166).