T7917

4'-Hydroxychalcone (2-Benzal-4-Hydroxyacetophenone) is a chalcone metabolite with hepatoprotective activity

Immuno modulator-1 (compound 22) effectively suppresses the secretion of TNFα and IL-2 in human peripheral blood mononuclear cells (hPBMC), with IC50 values of 4.7 nM and 26 nM, respectively, and exhibits a 20% inhibitory effect on the hERG potassium channel at a concentration of 3 μM [1].

Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor with an IC50 of 0.9 nM and minimal inhibition against Bcl-xl (IC50 > 1000 nM). It is used in cancer research related to Bcl-2 family protein overexpression, particularly in hematologic malignancies like acute lymphoid leukemia, while minimizing the risk of side effects such as thrombocytopenia [1] by sparing Bcl-xl.

PF-06655075 is a novel, non-brain-penetrant oxytocin receptor agonist that demonstrates enhanced selectivity for the oxytocin receptor and substantially improved pharmacokinetic stability. This compound serves as a tool to further investigate the function of peripheral oxytocin in behavioral responses [1].

PF-06478939 is a peptide that functions as an agonist at the oxytocin (OT) receptor and vasopressin receptor without crossing the blood-brain barrier. It exhibits EC50 values of 0.01 nM at the OT receptor and 0.078 nM at the vasopressin receptor [1].

PF-06478939 TFA is a peptide that acts as a non-brain-penetrating agonist at the oxytocin (OT) and vasopressin receptors, exhibiting EC50 values of 0.01 nM and 0.078 nM, respectively [1].

URAT1 inhibitor 6 (Compound 1h), with an IC50 of 35 nM for hURAT1, demonstrates 200-fold and 8-fold greater potency compared to Lesinurad and Benzbromarone, respectively. This compound is utilized in the study of inflammation [1].

Compound BDEO (URAT1&XO inhibitor 2) serves as a dual-action inhibitor targeting both xanthine oxidase (XO) and URAT1, demonstrating an IC50 value of 3.3 μM for XO inhibition. It effectively impedes uric acid uptake in HEK293 cells with URAT1 expression, evidenced by a Ki of 0.145 μM. In hyperuricemic mice models, the compound has been shown to reduce serum urate levels and uric acid excretion, indicating potential utility for hyperuricemia research [1].

WRN Inhibitor 2 (example 118), a potent inhibitor of the WRN (Werner Syndrome ATP-dependent helicase enzyme), exhibits a pIC50 value of 7.0 or greater [1].

GLX481304 is a selective Nox-2 and Nox-4 inhibitor, exhibiting IC50 values of 1.25 μM. It inhibits ROS production in isolated mouse cardiomyocytes and enhances their contractility. This compound is useful in research focused on ischemic cardiac injury [1].