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Cat No. | Product Name | Synonyms | Targets |
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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 |
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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... |
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... |