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Search Results for " pxr "

Targets

14

Compounds

8

Natural Products

2

Recombinant Proteins

Cat No. Product Name Synonyms Targets
T41255 Specific PXR antagonist 70 Others
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.
T21818 Pregnenolone Carbonitrile Pregnenolone 16α-carbonitrile ,5-Pregnen-3β-ol-20-one-16α-carbonitrile P450
Pregnenolone Carbonitrile (5-Pregnen-3β-ol-20-one-16α-carbonitrile) is an activator of rodent-PXR and induces the expression of CYP3A.
T6994 SR12813 SR-12813,SR 12813,GW 485801 HMG-CoA Reductase , Autophagy
SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist.
T4983 Isoetharine mesylate salt Isoetarine mesilate Others , Adrenergic Receptor
Isoetharine mesylate salt (Isoetarine mesilate) is a β-adrenergic receptor agonist. it also is pregnane X receptor (PXR) activator capable of upregulating CYP450 expression.
TP1313L Cecropin B acetate Cecropin B acetate(80451-05-4 Free base) P450 , Retinoid Receptor , Parasite
Cecropin B acetate induces NF-κB activation and suppresses CYP3A29 by disrupting the association of the PXR/retinoid X receptor alpha (RXR-α) complex with DNA sequences. Cecropin B acetate exhibits strong antimicrobial a...
T14973 CITCO Apoptosis , Others
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 al...
T67791 BMS-903452 GPR
BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestin...
T73265 Tolindate
Tolindate, a potent PXR agonist, demonstrates antifungal activity and possesses an EC50 value of 8.3 µM.
T30538 BMS-695735 CHEMBL459729,DNC008930,BMS 695735,BMS695735,BDBM27888
BMS-695735, a benzimidazole inhibitor of insulin-like growth factor-1 receptor, has broad-spectrum antitumor activity in vivo. It was found that BMS-695735 had strong inhibition of CYP3A4, induction of CYP3A4 mediated by...
T64116 B-Raf IN 5
B-Raf IN 5 is a potent inhibitor of the protein kinase B-Raf (IC50: 2.0 nM). B-Raf IN 5 resists rapid metabolism and does not bind to the secondary target PXR.
T70387 CCCTP
CCCTP is a potent inhibitor of the 11β-HSD-1 enzyme with reduced pregnane-X receptor (PXR) transactivation activity.
T63855 B-Raf IN 6
B-Raf IN 6 is a potent inhibitor (IC50: 1.7 nM) of the protein kinase B-Raf, which does not bind the secondary target PXR and is resistant to rapid metabolism.B-Raf IN 6 has shown research potential in cancer diseases.
T37351 Desmethyl Bosentan
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan .1Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in ...
T83765 Dendrogenin A ​DDA
Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholest...
Cat No. Product Name Synonyms Targets
T7974 Lynestrenol Progesterone Receptor
Lynestrenol is a synthetic progestational hormone, is the progesterone receptor agonist
T2939 Forskolin Coleonol,Colforsin FXR , Adenylyl cyclase , AChR , Autophagy
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...
T5S0734 Desmethoxyyangonin Desmethoxy yangonin,Demethoxyyangonin,5,6-Dehydrokavain Others , Monoamine Oxidase
1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS/D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK/NFκB and Jak2/STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydr...
T3797 Isosilybin Isosilybinin,Isosilibinin,Silymarin,Silybin B,Q-100795 P450
Isosilybin (Isosilibinin) and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.
T5813 BYAKANGELICIN Reductase
BYAKANGELICIN,a main furanocoumarin constituent isolated and characterized as an aldose reductase inhibitor,and is effective for the treatment of sugar cataracts and diabetic neuropathy and hence might be useful as a lea...
T4S1421 Praeruptorin B Praeruptorin D NPC1L1 , Fatty Acid Synthase
Praeruptorin B is an inhibitor of sterol regulatory element-binding proteins (SREBPs). It can also significantly up-regulate CYP3A4 expression and activity via the PXR-mediated pathway.
T10196 7α-Hydroxy-4-cholesten-3-one Others
7α-Hydroxy-4-cholesten-3-one is an intermediate in the synthesis of bile acids from cholesterol. It is a PXR agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss and other diseases associated with def...
TN1790 Isopteropodine Uncarine E 5-HT Receptor , Antibacterial , AChR
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 activi...

Recombinant Proteins

Cat No. Product Name Species Expression System
TMPY-02987 Vitamin D Receptor/VDR Protein, Mouse, Recombinant (His) Mouse Baculovirus-Insect Cells
VDR (vitamin D (1,25- dihydroxyvitamin D3) receptor), also known as NR1I1, belongs to the NR1I family, NR1 subfamily. It is composed of three domains: a modulating N-terminal domain, a DNA-binding domain and a C-terminal...
TMPY-02706 Vitamin D Receptor/VDR Protein, Human, Recombinant (His) Human Baculovirus-Insect Cells
VDR (vitamin D (1,25- dihydroxyvitamin D3) receptor), also known as NR1I1, belongs to the NR1I family, NR1 subfamily. It is composed of three domains: a modulating N-terminal domain, a DNA-binding domain and a C-terminal...
TargetMol