pxr

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a toxic secondary bile acid, They were FXR antagonists (IC50=0.7, 1.4 μM), EphA2 antagonists (IC50=48, 66 μM) and EphB4 antagonists (IC50=141 μM). Lithocholic acid can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is a cleanser that dissolves fat for absorption and is itself absorbed.

Helicid (Helicide) is a medicine available in a number of countries worldwide.

7α-Hydroxy-4-cholesten-3-one is an intermediate in bile acid synthesis from cholesterol, a PXR agonist, and a biomarker for bile acid loss and diseases related to defective bile acid biosynthesis. It is also the physiological substrate for [CYP8B1].

CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors. CITCO is an imidazothiazole derivative and it also is a selective Constitutive androstane receptor (CAR) agonist.

Pregnenolone Carbonitrile (5-Pregnen-3β-ol-20-one-16α-carbonitrile) is an activator of rodent-PXR and induces the expression of CYP3A.

Isopteropodine (Uncarine E) is an isoyohimbine-type octindole alkaloid isolated from Hamelia patens micropropagated and has antimicrobial activity and stimulates the immune system. Isopteropodine has antimicrobial activity and stimulates the immune system.Isopteropodine is a positive modulator of muscarinic M1 and 5-HT2 receptors and a PXR activator that induces contraction of the rat myometrium.

PXR Ligand 3 is a PXP ligand utilized in the synthesis of PROTACMI1013.

PXR ligand-Linker Conjugate 1 is a conjugate of a PXR ligand and a linker, suitable for synthesizing [PROTACMI1013].

Specific PXR antagonist 70 is a selective pregnane X receptor (PXR) antagonist with an IC50 of 540 nM and Ki of 390 nM for human PCR and enhances the chemosensitivity of cancer cells.

Lynestrenol is a synthetic progestational hormone, is the progesterone receptor agonist

Isoetharine mesylate salt (Isoetarine mesilate) is a β-adrenergic receptor agonist. it also is pregnane X receptor (PXR) activator capable of upregulating CYP450 expression.

BMS-903452 is a potent and selective GPR119 agonist with an EC50 of 14 nM, indicated for the treatment of acute and chronic rodent diabetes. GPR119 is mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. BMS-903452 shows no significant inhibitory effect on 9 cytochrome P450 enzymes (IC50 > 40 μM), does not activate PXR (EC50 > 50 μM), and is not toxic to liver (HEPG2) cell lines.

Diethanolamine hydrochloride has a variety of biological activities and is an inhibitor of HSD17B4 (hydroxysteroid 17-beta dehydrogenase 4) and pregnane X receptor (PXR), as well as an agonist of p53 and an antagonist of Estrogen receptor.

SJYHJ-026 (compound 37) is a pregnane X receptor (PXR) degrader with a DC50 value of 86.6 nM and a maximum degradation efficacy of 66.4%. This compound demonstrates cytotoxicity in SNU-C4 HiBiT-PXR KI cells, with IC50 values of 97.4 μM (24 h) and 99.5 μM (72 h).

PROTAC SMARCA2/4-degrader-34 (compound 38) serves as an effective degrader of both SMARCA2 and SMARCA4. It demonstrates binding affinity to PXR with a DC50 value of 85.1 nM and reduces the protein expression of 3xFLAG-PXR.

SJPUT-328 is a potent activator of the Pregnane X Receptor (PXR), which plays a crucial role in drug metabolism and drug interactions.

FKK6 is a selective agonist of the pregnane X receptor (PXR) with an EC50 of 1.2 µM. It demonstrates strong affinity for plasma proteins and exhibits favorable metabolic characteristics in human microsomes. FKK6 inhibits the PXR-related NF-κB signaling pathway, reducing the expression of inflammatory factors and showing anti-inflammatory activity in a mouse model of DSS-induced colitis.

SJPYT-310 is a selective PXR antagonist, exhibiting no noticeable cytotoxicity.

MI-883 is an orally active Constitutive Androstane Receptor (CAR, EC50=73 nM) agonist and a Pregnane X Receptor (PXR, IC50=0.1 μM) antagonist. It enhances CAR LBD assembly (EC50=0.38 µM) and activates the CAR3 variant (EC50=0.074 µM), inducing CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. Additionally, MI-883 inhibits the basal activity of PXR (IC50=2.03 µM) and reduces CYP3A4 mRNA expression in transiently transfected HepG2 cells. It also regulates cholesterol metabolism and bile acid excretion, improving hypercholesterolemia in mouse models.

Cholic acid-Glu is a derivative of Cholic acid. Its abundance rises in Crohn's disease. This compound can enhance the activation of PXR in intestinal organoid tissues and significantly increase the expression of the downstream PXR target gene, Cyp3a11.

MI891 is a highly selective PXR antagonist (IC50= 3.76 μM, Kd= 1.7 μM) and inverse agonist (IC50= 6.1 μM). It selectively disrupts the interaction between PXR and its coactivator SRC1. MI891 effectively inhibits Rifampicin-induced PXR activation and can be utilized in research on metabolic and other diseases.

MI1013 is a PROTAC PXR degrader with a DC50 of 89 nM and a Dmax of 82%. It degrades PXR in human liver cancer RG cells (HepaRG) and modulates CYP3A4 promoter activity with specificity and safety through PXR degradation. MI1013 influences key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketogenesis (HMGCS20), and hepatocyte proliferation (MKI67).

Benzophenone-2 (2,2',4,4'-Tetrahydroxybenzophenone) is an endocrine disruptor that targets the pregnane X receptor (PXR) and estrogen receptor α (ERα). It modulates the expression of cytochrome P450 3A (CYP3A) by activating PXR. Benzophenone-2 is promising for research in UV filters.