Pregnane X Receptor (PXR) Agonist

FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12^F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12^F36V, without degrading wild-type FKBP12 or un-fused PXR. It weakly promotes the recruitment of SRC-1, strongly inhibits the interaction between NCoR and PXR, and upregulates the expression of CYP3A4 and other drug metabolism-related genes. FKBP12 PROTAC dTAG-13 is applicable to research related to breast cancer and leukemia^[1].

SR12813 (GW 485801) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC₅₀ value of 0.85 μM. SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR).

Lynestrenol (Standard) is the analytical standard of Lynestrenol. This product is intended for research and analytical applications. Lynestrenol is a pregnane X receptor (PXR) agonist with the EC50s of 41 and 0.23 μM for hPXR and zfPXR, respectively. Lynestrenol, a synthetic progesteronelike agent possess immunostimulatory properties.

Lynestrenol is a pregnane X receptor (PXR) agonist with the EC₅₀s of 41 and 0.23 μM for hPXR and zfPXR, respectively. Lynestrenol, a synthetic progesteronelike agent possess immunostimulatory properties.

4,8-Dioxa-3H-perfluorononanoic acid is an ether-substituted polyfluoroalkyl compound and also a ligand of human pregnane X receptor (hPXR), which binds to the ligand-binding domain of hPXR. 4,8-Dioxa-3H-perfluorononanoic acid targets Arg-410, Lys-210, Lys-226, Met-323 and His-327 residues. Its binding process relies on long-range electrostatic interactions, and no significant hydrogen bonds form with hPXR residues. 4,8-Dioxa-3H-perfluorononanoic acid is used as a substitute for PFOA in Germany. 4,8-Dioxa-3H-perfluorononanoic acid is detectable in environmental matrices such as river water near fluoride production plants, accumulates in organisms including grass, deer liver and locusts, and is present in plasma samples of populations in southern Germany.

Garcinoic acid is an orally active anti-inflammatory agent that crosses the blood-brain barrier. Garcinoic acid also enhances efferocytosis and enzyme/receptor regulation, and selectively inhibits human COX-2, porcine α-amylase, Saccharomyces cerevisiae α-glucosidase and human DNA polymerase β (IC₅₀=11 μM), as well as activates human PXR. Garcinoic acid enhances macrophage efferocytosis via receptors such as MerTK and LRP-1, and promotes the production of pro-resolving lipid mediators. Garcinoic acid inhibits NF-κB activation and pro-inflammatory cytokine secretion, interferes with Aβ aggregation, downregulates NLRP3 inflammasome activity, and binds to targets including CD44 and EGFR to inhibit leukemia cell proliferation. The pharmacological activities of Garcinoic acid, such as antioxidant, anti-inflammatory and lipid metabolism-regulating effects, are widely used in studies related to various diseases including atherosclerosis, Alzheimer's disease, type 2 diabetes, inflammatory bowel disease and viral pneumonia.

SJB7 is a pregnane X receptor (PXR) agonist. SJB7 can stabilize the activation function 2 (AF-2) helix in an “inward” position.

N-Cholyl-L-threonine (ThrCA) is a Cholic acid (HY-N0324) conjugated with L-threonine (HY-N0658). N-Cholyl-L-threonine possesses PXR agonism activity. N-Cholyl-L-threonine can be used in the research of Crohn's disease.

SJPYT-328 is a PXR agonsit. PXR plays a major role in drug metabolism and drug-drug interactions.

SR12813 (Standard) is the analytical standard of SR12813 (HY-100793). This product is intended for research and analytical applications. SR12813 (GW 485801) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM. SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR).

Tolindate is a potent PXR agonist with an EC₅₀ value of 8.3 μM. Tolindate shows antifungal activity.