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UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders .
UGT1A1-IN-1 (compound 2) is a non-competitive inhibitor of UGT1A1, which can inhibit the 1-O-glucuronidation process mediated by UGT1A1 with a Ki value of 5.02 μM. UGT1A1-IN-1 (compound 2) can bind on UGT1A1 at the same ligand-binding site as bilirubin (HY-N0323). UGT1A1-IN-1 can serve as a ‘turn-on’ fluorescent probe substrate for UGT1A1 .
Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation .
Trifluoperazine N-glucuronide (UGT1A4) chloride is a metabolite of the antipsychotic agent trifluoperazine. Trifluoperazine N-glucuronide (UGT1A4) chloridecatalyzes the imipramine and trifluoperazine Nglucuronide formation .
UGT8 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A1 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A10 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A10 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A3 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A4 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A6 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A7 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A8 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT1A9 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2A1 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2A2 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2A2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2A3 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2A3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT3A2 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT3A2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2B10 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2B10 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2B15 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2B15 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2B17 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2B17 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2B4 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2B4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UGT2B7 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT2B7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes .
RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation .
Licochalcone A (LCA), a flavonoid isolated, presents obvious anti-cancer effects, displays broad-spectrum inhibition against UDP-glucuronosyltransferases (UGTs) . Licochalcone A (LCA) exhibits strong inhibitory effects against UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A9, and 2B7 (both IC50 and Ki values lower than 5 μM) .
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
Hesperetin-d3 is the deuterium labeled Hesperetin[1]. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin regulates apoptosis[2][3].
Carlinoside is a flavone glycoside with hepatoprotective efficiency. Carlinoside reduces hepatic bilirubin accumulation by stimulating bilirubin-UGT activity through Nrf2 gene expression. Carlinoside has the potential to intervene hyperbilirubinemia due to liver dysfunction .
Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
(Rac)-Hesperetin-d3 is the deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca 2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme .
(Rac)-Hesperetin- 13C,d3 is the 13C- and deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS .
Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS .
Cabotegravir (Standard) is the analytical standard of Cabotegravir. This product is intended for research and analytical applications. Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS .
4-Hydroxyretinoic acid (4-HRA) is a naturally occurring retinoid derivative with diverse biological effects. 4-Hydroxyretinoic acid is formed from retinol catalyzed by cytochrome P-450 isozyme(s), and is mainly metabolized by the liver in the body. 4-Hydroxyretinoic acid also serves as the substrate for human liver microsomal UDP-glucuronosyltransferase(s) and recombinant UGT2B7. 4-Hydroxyretinoic acid regulates gene expression and cell differentiation via binding to nuclear receptor RAR (Retinoic Acid Receptor), and activates RARs and RXR-alpha, to induce cancer cell apoptosis. In addition, 4-Hydroxyretinoic acid is also involved in various physiological processes such as immune regulation, neuroprotection, and anti-oxidation .
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes .
Licochalcone A (LCA), a flavonoid isolated, presents obvious anti-cancer effects, displays broad-spectrum inhibition against UDP-glucuronosyltransferases (UGTs) . Licochalcone A (LCA) exhibits strong inhibitory effects against UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A9, and 2B7 (both IC50 and Ki values lower than 5 μM) .
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
Carlinoside is a flavone glycoside with hepatoprotective efficiency. Carlinoside reduces hepatic bilirubin accumulation by stimulating bilirubin-UGT activity through Nrf2 gene expression. Carlinoside has the potential to intervene hyperbilirubinemia due to liver dysfunction .
Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca 2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme .
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
The UGT1A1 protein is an important UDP-glucuronosyltransferase (UGT) that drives phase II biotransformation by conjugating lipophilic substrates with glucuronic acid, enhancing water solubility, and promoting excretion. UGT1A1 is critical for the elimination of drugs, xenobiotics, and endogenous compounds and exhibits multiple substrate specificities, glucuronidating estrogens, bilirubin, phytoestrogens such as genistein and daidzein, and SN -38. UGT1A1 Protein, Human (P.pastoris, His) is the recombinant human-derived UGT1A1 protein, expressed by P. pastoris , with N-6*His labeled tag.
SLC35A2 is a key transmembrane protein that acts as an antiporter to transport uridine diphosphate galactose (UDP-galactose) into the Golgi apparatus. The process involves the exchange of UDP-galactose with UMP and exhibits versatility through exchange with AMP and CMP. SLC35A2 Protein, Human (Sf9, His, MBP, FLAG) is the recombinant human-derived SLC35A2 protein, expressed by Sf9 insect cells , with N-MBP, C-Flag, N-8*His labeled tag. The total length of SLC35A2 Protein, Human (Sf9, His, MBP, FLAG) is 395 a.a., .
Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
Hesperetin-d3 is the deuterium labeled Hesperetin[1]. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin regulates apoptosis[2][3].
Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
(Rac)-Hesperetin-d3 is the deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
(Rac)-Hesperetin- 13C,d3 is the 13C- and deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
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