cyp3a4-in-2

CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) (IC50: 0.055 μM). As a ritonavir analogue with a more hydrophobic R2 side group, CYP3A4-IN-2 exhibits stronger inhibition than ritonavir and is capable of acting as an immunosuppressive and antiviral agent.

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.

TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin that induces apoptosis. This compound enhances the expression of p53, caspase-3, caspase-8, caspase-9, and Bax proteins, while reducing Bcl-2 protein levels. TCF4/β-catenin-IN-1 also inhibits CYP3A4, CYP1A2, and CYP2C19, demonstrating significant cytotoxic activity in cancer cells.

EGFR/DHFR-IN-2 (9b) is a dual inhibitor of h-DHFR/EGFR TK, exhibiting IC50 values of 0.192 μM for h-DHFR and 0.109 μM for EGFR. It causes cell cycle arrest at the G1/S phase and induces apoptosis. Additionally, EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. This compound can be utilized in cancer research.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

Clindamycin sulfoxide, an active metabolite of the antibiotic clindamycin, is formed via S-oxidation primarily by the cytochrome P450 (CYP) isoform CYP3A4. It inhibits the growth of P. prevotti, B. fragilis, and C. sordelli in vitro with MIC values of 2, 2, and 1 mg/L, respectively.

Imidafenacin metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist imidafenacin.1It is formed from imidafenacin by the cytochrome P450 (CYP) isoform CYP3A4. 1.Kanayama, N., Kanari, C., Masuda, Y., et al.Drug-drug interactions in the metabolism of imidafenacin: Role of the human cytochrome P450 enzymes and UDP-glucuronic acid transferases, and potential of imidafenacin to inhibit human cytochrome P450 enzymesXenobiotica37(2)139-154(2007)

Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine. It is formed by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes from HepG2 cells expressing CYP3A4 or CYP2C8, respectively. Carbamazepine 10,11-epoxide exhibits anticonvulsant activity against maximal electroshock-induced seizures in mice and has been detected in wastewater effluent [1][2][3].

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist with a K_i of 0.66 nM, which does not interact with CYP3A4 and demonstrates potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

5-hydroxy Omeprazole is one of the major metabolites of the proton pump inhibitor omeprazole in the body; it is formed by hydroxylation catalyzed by the CYP2C19 and CYP3A4 enzymes in the liver. 5-hydroxy Omeprazole can be used in pharmacokinetic studies.

6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 μM). 6'7'-Epoxybergamottin also has insecticidal properties with a concentration of 5 μg/cm2 leading to 100% mortality of adult olive fruit flies.

1. Resibufogenin (Bufogenin) is a cytotoxic steroid isolated from the Chinese drug ChanSu. 2. Resibufogenin can inhibit rectifier potassium current ( I K ) and transient potassium current ( I A ), it has pathological effects on central nervous system. 3. Resibufogenin corrects hypertension in a rat model of human preeclampsia, it not only prevents the advent of hypertension and proteinuria, but also the development of intrauterine growth restriction.4. Resibufogenina's major metabolic pathway in the human liver is CYP3A4 dominantly mediated 5β-hydroxylation .

1. Neferine ((-)-Neferine) has anti-tumor activities , Metabolic activation mediated by CYP3A4 and GSH depletion enhanced Neferine-induced cytotoxicity. 2. Neferine can be helpful to increase the efficacy of DOX and to achieve anticancer synergism by curbing the toxicity. 3. Neferine inhibited high glucose-induced endothelial apoptosis via blocking ROS/Akt/NF-κB pathway, which provides the evidence for using Neferine to treat diabetic vasculopathy. 4. Neferine induced apoptosis in a dose-dependent manner with the hypergeneration of reactive oxygen species, activation of MAPKs, lipid peroxidation, depletion of cellular antioxidant pool, loss of mitochondrial membrane potential, and intracellular calcium accumulation.

Carbamazepine-10,11-epoxide-D10 (rings-D10) is a deuterated compound of Carbamazepine-10,11-epoxide. Carbamazepine-10,11-epoxide (T37149) has a CAS number of 36507-30-9. Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine[1][2].It is formed from carbamazepine by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes prepared from HepG2 cells expressing CYP3A4 or CYP2C8, respectively[1].Carbamazepine 10,11-epoxide has anticonvulsant activity against maximal electroshock-induced seizures in mice.2It has been found in wastewater effluent[3].

Terfenadine (Standard) is the standard substance of Terfenadine, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Terfenadine ((±)-Terfenadine) is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistaminic and non-sedative effects.

Ginsenoside Rd (Standard) is a reference standard for research and analysis in studies involving Ginsenoside Rd. Ginsenoside Rd (Gypenoside VIII) may have properties that inhibit or prevent the growth of tumors.

Tetrahydrocurcumin (Standard) is a reference standard for research and analysis in studies involving Tetrahydrocurcumin. Tetrahydrocurcumin (HZIV 81-2), a major metabolite of curcumin, has strong antioxidant and cardioprotective properties.

Amentoflavone (Standard) is a reference standard for research and analysis in studies involving Amentoflavone. Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

Resibufogenin (Standard) is a reference standard for research and analysis in studies involving Resibufogenin. 1. Resibufogenin (Bufogenin) is a cytotoxic steroid isolated from the Chinese drug ChanSu. 2. Resibufogenin can inhibit rectifier potassium current ( I K ) and transient potassium current ( I A ), it has pathological effects on central nervous system. 3. Resibufogenin corrects hypertension in a rat model of human preeclampsia, it not only prevents the advent of hypertension and proteinuria, but also the development of intrauterine growth restriction.4. Resibufogenina's major metabolic pathway in the human liver is CYP3A4 dominantly mediated 5β-hydroxylation .

Carbamazepine 10,11-epoxide (Standard) is a reference standard for research and analysis in studies involving Carbamazepine 10,11-epoxide. Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine[1][2].It is formed from carbamazepine by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes prepared from HepG2 cells expressing CYP3A4 or CYP2C8, respectively[1].Carbamazepine 10,11-epoxide has anticonvulsant activity against maximal electroshock-induced seizures in mice.2It has been found in wastewater effluent[3].

Carbamazepine-10,11-Epoxide-D10 (Rings-D10) (Standard) is a reference standard of Carbamazepine-10,11-Epoxide-D10 (Rings-D10) intended for quantitative analysis, quality control, and related biochemical research applications. Carbamazepine-10,11-epoxide-d10 (rings-d10) is a deuterated compound of Carbamazepine-10,11-epoxide. Carbamazepine-10,11-epoxide has a CAS number of 36507-30-9. Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine[1][2].It is formed from carbamazepine by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes prepared from HepG2 cells expressing CYP3A4 or CYP2C8, respectively[1].Carbamazepine 10,11-epoxide has anticonvulsant activity against maximal electroshock-induced seizures in mice.2It has been found in wastewater effluent[3].