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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
18 Results for "
human pregnane X receptor
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "human pregnane X receptor" in MCE Product Catalog:
7
7 Publications Verification
Synonyms: GW 485801
Research Areas:
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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1 Cited Publications
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TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy .
Cat. No.: HY-W587839
CAS No.: 919005-14-4
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Research Areas:
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 .
Synonyms: TSH-888
Research Areas:
Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
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-173033
CAS No.: 2530027-71-3
Research Areas:
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-145516
CAS No.: 253688-61-8
Synonyms: Ro 47-8634
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Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.
Cat. No.: HY-134522
CAS No.: 2259710-64-8
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DL5050 is a selective and potent human constitutive androstane receptor (hCAR) agonist that does not activate pregnane X receptor (PXR). DL5050 preferentially induces the expression of CYP2B6 (target of hCAR) over CYP3A4 (target of hPXR) on both the mRNA and protein levels. DL5050 can be used for the researches of cancer and metabolic disease, such as diabetes .
Cat. No.: HY-100793R
CAS No.: 126411-39-0
Synonyms: GW 485801 (Standard)
Research Areas:
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) .
Cat. No.: HY-122163
CAS No.: 1149750-69-5
Research Areas:
MK-3901 is a selective P2X3 receptor antagonist with an IC50 of 24 nM. MK-3901 inhibits UGT1A1 (with an IC50 of 1 μM) and CYP2C9 (with an IC50 of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain .
Cat. No.: HY-E72107
Human UGT1A4 is a UDP-glucuronosyltransferase. Human UGT1A4 is the major enzyme catalyzing the glucuronidation of 25-hydroxyvitamin D3 (HY-32351) in the liver, and maintains vitamin D homeostasis by clearing 25-hydroxyvitamin D3. Human UGT1A4 regulates the substrate-dependent enzymatic activities of UGT1A1 and UGT1A6, while its own activity is also subject to substrate-dependent regulation by co-expressed UGT1A1 and UGT1A6 .
Cat. No.: HY-P701396
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: NR1I2; Steroid And Xenobiotic receptor; Nuclear receptor Subfamily 1 Group I Member 2; Orphan Nuclear receptor PAR1; Orphan Nuclear receptor PXR; Nuclear receptor Subfamily 1, Group I, Member 2; pregnane X receptor; PARq; PAR2; PAR1; SXR; SAR; PXR; PRR; O
Species:
Human
Source:
E. coli
Cat. No.: HY-P701397
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: NR1I2; Steroid And Xenobiotic receptor; Nuclear receptor Subfamily 1 Group I Member 2; Orphan Nuclear receptor PAR1; Orphan Nuclear receptor PXR; Nuclear receptor Subfamily 1, Group I, Member 2; pregnane X receptor; PARq; PAR2; PAR1; SXR; SAR; PXR; PRR; O
Species:
Human
Source:
E. coli
Cat. No.: HY-182582
CAS No.: 1430210-54-0
Research Areas:
ZY12201 is a selective and orally active TGR5 agonist and pan-CYP inhibitor. ZY12201 lowers glucose levels. ZY12201 induces enzymes regulated through Aryl Hydrocarbon Receptor, Constitutive Androstane Receptor, and Pregnane X Receptor. ZY12201 can be used for the research of type 2 diabetes .
Cat. No.: HY-182637
CAS No.: 1809863-68-0
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ACT-774312 is a potent and selective CRTH2 antagonist with an IC50 of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD2-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.
Cat. No.: HY-182928
CAS No.: 3018825-60-7
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LRRK2-IN-21 is a selective, blood-brain barrier-permeable LRRK2 kinase inhibitor with an IC50 of 0.35 nM. LRRK2-IN-21 inhibits TTK kinase with an IC50 of 70 nM. LRRK2-IN-21 is applicable to the research of Parkinson's disease .
Cat. No.: HY-111828R
CAS No.: 953778-63-7
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TTA-A2 (Standard) is the analytical standard of TTA-A2 (HY-111828). This product is intended for research and analytical applications. TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy .
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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
