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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
29 Results for "
PXR agonist
" in MedChemExpress (MCE) Product Catalog:
Products (29)
29 Results for "PXR agonist" in MCE Product Catalog:
21
21 Publications Verification
Synonyms: 3α-Hydroxy-5β-cholanic acid
Category:
Human Gut Microbiota Metabolites Anti-aging Metabolic Disease Endogenous metabolite Disease Research Fields Steroids
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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] .
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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) .
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3 Cited Publications
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. 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 .
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Cat. No.: HY-W015026
CAS No.: 4247-02-3
Synonyms: Isobutyl-P-Hydroxybenzoate
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Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics .
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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 .
Cat. No.: HY-168328
CAS No.: 2238839-34-2
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FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
Cat. No.: HY-148223
CAS No.: 27877-51-6
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Tolindate is a potent PXR agonist with an EC50 value of 8.3 μM. Tolindate shows antifungal activity .
Cat. No.: HY-W015026S
CAS No.: 1219805-33-0
Synonyms: Isobutyl 4-hydroxybenzoate-d4
Cat. No.: HY-178780
CAS No.: 2137977-29-6
Synonyms: MKP10241
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Deziglipel (MKP10241) is an orally active GPR119 agonist (human EC50: 3.7 nM; IC50 > 7.2 μM). Deziglipel activates GPR119 to increase cAMP levels, promotes active GLP-1 release, reduces blood glucose and HbA1c, decreases body weight and feed intake, and resolves MASH via altered lipid, cytokine, and liver enzyme levels. Deziglipel shows low hERG channel inhibition, minimal CYP450 inhibition, no PXR activation, and no significant transporter inhibition. Deziglipel can be used for the research of type 2 diabetes mellitus, obesity, MASH/MASLD, and metabolic disorders .
Cat. No.: HY-173033
CAS No.: 2530027-71-3
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MI-883 is orally active constitutive androstane receptor (CAR) (EC50 of 73 nM) agonist and pregnane X Receptor (PXR) (IC50 of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol, LDL cholesterol, and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia .
Cat. No.: HY-15380
CAS No.: 185220-03-5
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PNU-142721 is a reverse transcriptase inhibitor and PXR agonist that effectively inhibits various type I HIV variants .
Cat. No.: HY-175264
CAS No.: 2530027-77-9
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MI891 is a highly selective PXR antagonist (IC50 = 3.76 μM, Kd = 1.7 μM) and inverse agonist (IC50 = 6.1 μM). MI891 selectively disrupts the interaction between PXR and its coactivator SRC1. MI891 effectively inhibits Rifampicin (HY-B0272)-induced PXR activation. MI891 is useful for the study of metabolic diseases and other diseases .
Cat. No.: HY-18612
CAS No.: 1034152-93-6
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MK-7725 is a selective, orally active, and blood-brain barrier-permeable agonist of the subtype 3 of the frog skin peptide receptor (BRS-3). MK-7725 has a high affinity for the human BRS-3 (hBRS-3), with an IC50 of 3 nM, and its functional activity in the mouse-derived BRS-3 (mBRS-3) model with an EC50 of 22 nM (105% agonistic). MK-7725 significantly reduces the body weight of obese rats and obese dogs. MK-7725 can be used for the treatment of obesity .
Cat. No.: HY-179875
CAS No.: 22154-46-7
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N-Cholyl-L-leucine is a bile acid-amino acid conjugate, mainly produced by intestinal microorganisms. N-Cholyl-L-leucine can be used as a biomarker for premature infants and is also employed in the study of bile acid metabolism .
Cat. No.: HY-113259R
CAS No.: 3862-25-7
Cat. No.: HY-169279
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PROTAC PXR degrader-1 is a PROTAC degrader targeting PXR, with a DC50 value of 49.8 nM in SNU-C4 3xFLAG-PXR KI cells. PROTAC PXR degrader-1 exhibits selectivity towards CAR, VDR, FXR, LXRα and LXRβ. PROTAC PXR degrader-1 induces the formation of a ternary complex with PXR and VHL, triggering proteasomal degradation of PXR. PROTAC PXR degrader-1 reduces both agonist-induced and basal PXR-mediated CYP3A4 promoter activation, and decreases the expression of endogenous CYP3A4 gene in cancer cells. PROTAC PXR degrader-1 enhances the cytotoxic effect of paclitaxel on cancer cells. PROTAC PXR degrader-1 can be used for the research of colorectal cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
