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Lynestrenol is a pregnaneXreceptor(PXR) agonist with the EC50s of 41 and 0.23 μM for hPXR and zfPXR, respectively . Lynestrenol, a synthetic progesteronelike agent possess immunostimulatory properties .
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 pregnaneXreceptor(PXR), and no activity on other nuclear receptors .
Benzophenone-2 (2,2',4,4'-Tetrahydroxybenzophenone) is an endocrine disruptor targeting pregnaneXreceptor(PXR) and estrogen receptor α (ERα). Benzophenone-2 regulates cytochrome P450 3A (CYP3A) expression by activating PXR. Benzophenone-2 is promising for research of UV filters .
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnaneXreceptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnaneXreceptor(PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids .
FKK6 is a selective agonist for pregnaneXreceptor(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 .
(3S,5S)-Atorvastatin sodium salt is a pregnaneXreceptor(PXR) activator and the inactive enantiomer of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor with lipid-lowering capabilities .
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnaneXreceptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.
CaSR
antagonist-1 is a calcium sensing receptor (CaSR) antagonist
with an IC50 value of 50 nM. CaSR
antagonist-1 can be used for the research of disorders associated with abnormal
bone or mineral homeostasis such as osteoporosis .
Lynestrenol (Standard) is the analytical standard of Lynestrenol. This product is intended for research and analytical applications. Lynestrenol is a pregnaneXreceptor (PXR) agonist with the EC50s of 41 and 0.23 μM for hPXR and zfPXR, respectively . Lynestrenol, a synthetic progesteronelike agent possess immunostimulatory properties .
SJYHJ-026 (compound 37) is a pregnaneXreceptor(PXR) PROTAC degrader with the DC50 of 86.6 nM and maximal degradation of 66.4%. SJYHJ-026 shows cell cytotoxic aganist SNU-C4 HiBiT-PXR KI cells with the IC50 values of 97.4 μM (24 h) and 99.5 μM (72 h) (Blue: VHL ligand HY-125845,Black: linker HY-43048；Pink: PXR inhibitor HY-169277) .
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 pregnaneXreceptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR) .
JMV7048 is an effective PROTAC degrader targeting PXR (PregnaneXReceptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker) .
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnaneXreceptor(PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin (GMP) is also an inducer of intracellular cAMP formation . Forskolin (GMP) induces differentiation of various cell types and activates pregnaneXreceptor(PXR) and FXR . Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy .
Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnaneXreceptor (PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for PregnaneXReceptor(PXR,IC50=0.1 μM). MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnaneXreceptor (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 .
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnaneXreceptor(PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
7α-Hydroxy-4-cholesten-3-one-d7 is the deuterium labeled 7α-Hydroxy-4-cholesten-3-one. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnaneXreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
7α-Hydroxy-4-cholesten-3-one (Standard) is the analytical standard of 7α-Hydroxy-4-cholesten-3-one. This product is intended for research and analytical applications. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnaneXreceptor(PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
BODIPY-FL-Vindoline is a high-affinity fluorescent probe for the pregnaneXreceptor(PXR), with a Kd of 256 nM. BODIPY-FL-Vindoline can be used in the research of drug metabolism and drug-drug interactions .
Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin (GMP) is also an inducer of intracellular cAMP formation . Forskolin (GMP) induces differentiation of various cell types and activates pregnaneXreceptor(PXR) and FXR . Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy .
Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin (GMP) is also an inducer of intracellular cAMP formation . Forskolin (GMP) induces differentiation of various cell types and activates pregnaneXreceptor(PXR) and FXR . Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy .
Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnaneXreceptor(PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnaneXreceptor (PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnaneXreceptor(PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
7α-Hydroxy-4-cholesten-3-one (Standard) is the analytical standard of 7α-Hydroxy-4-cholesten-3-one. This product is intended for research and analytical applications. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnaneXreceptor(PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
NR1I2; Nuclear receptor subfamily 1 group I member 2; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; pregnane X receptor; Steroid and xenobiotic receptor; SXR
The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human (His) is the recombinant human-derived PXR protein, expressed by E. coli , with N-6*His labeled tag.
NR1I2; Nuclear receptor subfamily 1 group I member 2; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; pregnane X receptor; Steroid and xenobiotic receptor; SXR
The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human is the recombinant human-derived PXR protein, expressed by E. coli , with tag free.
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
7α-Hydroxy-4-cholesten-3-one-d7 is the deuterium labeled 7α-Hydroxy-4-cholesten-3-one. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnaneXreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnaneXreceptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
FKK6 is a selective agonist for pregnaneXreceptor(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 .
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