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(S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochromeP450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochromeP450 metabolism .
7-Ethoxycoumarin-d5 is deuterium labeled 7-Ethoxycoumarin. 7-Ethoxycoumarin is a substrate for cytochromeP450(CYP450) and has been used in the functional characterization of various CYPs[1].
RPR132595A (NPC) hydrochloride is an active metabolite of CPT-11, which is generated by cytochromeP-450 3A4 (CYP3A4) and finally excreted through urine .
Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochromeP450 (CYP) enzymes, e.g., CYP2C .
18-HETE (compound 3) is a monooxygenase metabolite of cytochromeP450 (CYP450).18- HETE consists of arachidonic acid bearing a hydroxy substituent at position 18 .
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochromeP450(CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochromeP450 2A6 (CYP2A6) .
Tienilic acid (Ticrynafen; ANP 3624) acts as a diuretic hypotensive agent. However, Tienilic acid induces hepatotoxicity. Tienilic acid is converted into electrophilic metabolites by cytochromeP450 (CYP) in vitro .
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochromeP450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
Resorufin methyl ether (Methoxyresorufin) is a cytochromeP450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .
Clotrimazole-d5 is the deuterium labeled Clotrimazole. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochromeP450) inhibitor. Clotrimazole has antibacterial activity[1][2].
Clotrimazole (Standard) is the analytical standard of Clotrimazole. This product is intended for research and analytical applications. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochromeP450) inhibitor. Clotrimazole has antibacterial activity.
Clotrimazole-d10 is deuterated labeled Clotrimazole (HY-10882). Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochromeP450) inhibitor. Clotrimazole has antibacterial activity.
Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochromeP450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp .
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochromeP450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
Cobicistat is a potent and selective inhibitor of cytochromeP450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochromeP450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochromeP450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
6-Hydroxywarfarin is a metabolite of (+) -warfarin. 6-Hydroxywarfarin is a weaker vitamin K antagonist. 6-Hydroxywarfarin is metabolized by the cytochromeP450 isomer 2C9 (CYP2C9) .
Isonicotinic acid-d4 is the deuterium labeled Isonicotinic acid[1]. Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochromeP450 (CYP) enzymes, e.g., CYP2C[2].
Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochromep450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a metabolite of Xanthotoxin. Xanthotoxin is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochromeP-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight .
Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochromeP-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochromeP450 enzymes CYP1A2 in human liver microsomes and in rats .
2-Naphthol-d8 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochromeP450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
2-Naphthol-d7 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochromeP450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochromeP450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochromeP450 (CYP) 1A1 activity .
Anticancer agent 111 (compound 11) is a potent cytochromeP450 inhibitor with an IC50 value of 3 μM for CYP3A4. Anticancer agent 111 has anticancer activity. Anticancer agent 111 can be used in research of cancer .
4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochromeP450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties .
Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochromeP-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke .
Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochromep450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
CYP3A4-IN-3 is a high-affinity specific inhibitor of cytochromeP450 3A4 (CYP3A4) with the IC50 value of 0.075 μM. CYP3A4-IN-3 is a ritonavir analogue, but with a simpler structure and twice the inhibitory effect of ritonavir. CYP3A4-IN-3 is used as an antiviral agent and immunosuppressant .
CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochromeP450 (CYP) 4A11 and CYP4F2, with IC50s of 19 nM and 17 nM, respectively. CYP4A11/CYP4F2-IN-1 has potential for the research of renal diseases .
Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochromeP450 3A (CYP3A) enzymes[1][2].
CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochromeP450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases .
CYP3A4-IN-2 is a specific inhibitor of cytochromeP450 3A4 (CYP3A4) with the IC50 value of 0.055 μM. CYP3A4-IN-2 is a ritonavir analogue with increased hydrophobicity of the R2 side group and stronger inhibitory effect compared to ritonavir. CYP3A4-IN-2 can be used as an antiviral agent and immunosuppressants .
Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP(cytochromeP450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis .
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochromeP450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochromeP450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties .
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochromeP450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
5-Methyl-2-furanmethanol is a natural product that can be isolated from the essential oil of D. rupicola Biv.. 5-Methyl-2-furanmethanol also acts as a oxidative product of 2,5 dimethylfuran (DMF) by cytochromeP450 (CYP) .
Fomepizole (4-Methylpyrazole) is a potent cytochromeP450(CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochromeP450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochromeP450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties .
MS-PPOH is a potent and selective cytochromeP450(CYP)epoxygenase inhibitor . MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 μM, respectively . MS-PPOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochromeP450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .
Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochromeP450(CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning .
Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochromeP450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
Phenacetin (Standard) is the analytical standard of Phenacetin. This product is intended for research and analytical applications. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochromeP450 enzymes CYP1A2 in human liver microsomes and in rats .
Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochromeP-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM . Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM) . Kushenol K also inhibits the activity of SGLT1 and SGLT2 .
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
4-Hydroxyatomoxetine-d3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochromeP450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor[1].
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochromeP450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochromeP450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochromeP450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity .
Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochromeP450 (CYP) 2C9 and CYP3A .
Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochromeP450 (CYP) 2C9 and CYP3A .
Avatrombopag maleate (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag maleate mimics the biological activities of TPO. Avatrombopag maleate increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag maleate is a substrate of cytochromeP450 (CYP) 2C9 and CYP3A .
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochromeP-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochromeP450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm,Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
(±)-N-3-Benzylnirvanol is a racemic mixture of (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol. (+)-N-3-Benzylnirvanol and (–)-N-3-Benzylnirvanol are potent and selective cytochromeP450 inhibitors with Ki values of 0.25 and 5.3 μM for CYP2C19, respectively .
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochromeP450 (CYP) isoform CYP3A in human liver microsomes.
4'-Hydroxy diclofenac-d4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochromeP450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[1][2].
Chlorzoxazone-d3 is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochromeP450 2E1 (CYP2E1) activity in humans.
Hypericin (Standard) is the analytical standard of Hypericin. This product is intended for research and analytical applications. Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP(cytochromeP450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis .
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochromeP450 (CYP) 2C9 and CYP3A[1][2][3].
FGFR-IN-10 is an orally active inhibitor of FGFR and CytochromeP450(CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively .
4'-Hydroxy diclofenac- 13C6 is the 13C labeled 4'-Hydroxy diclofenac[1]. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochromeP450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[2][3].
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochromeP450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochromeP450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochromeP450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the CytochromeP450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth .
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochromeP450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
Sulfaphenazole is a selective inhibitor of human cytochromeP450 (CYP) 2C9 enzyme. Sulfaphenazole is a cytoprotective agent against light-induced death of photoreceptors. Sulfaphenazole inhibits light-induced necrosis and mitochondrial stress-initiated apoptosis. Sulfaphenazole is an off patent sulfonamide antibiotic and demonstrates bactericidal activity through enhanced M1 macrophage activity. Sulfaphenazole can significantly reduce infarct size and restore post-ischemic coronary flow following ischemia and reperfusion .
GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochromeP450, CYP3A4 isoform .
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochromeP450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor) .
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochromeP450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochromeP450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochromeP450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochromeP450(CYP450) .
Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochromeP450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and cytochromeP450 (CYP) 2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation .
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
Resorufin methyl ether (Methoxyresorufin) is a cytochromeP450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochromeP450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochromeP450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm,Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochromeP450 (CYP) enzymes, e.g., CYP2C .
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochromeP450(CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochromeP450 2A6 (CYP2A6) .
Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochromeP450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp .
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochromeP450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a metabolite of Xanthotoxin. Xanthotoxin is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochromeP-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight .
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochromeP450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochromeP450 (CYP) 1A1 activity .
Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP(cytochromeP450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis .
5-Methyl-2-furanmethanol is a natural product that can be isolated from the essential oil of D. rupicola Biv.. 5-Methyl-2-furanmethanol also acts as a oxidative product of 2,5 dimethylfuran (DMF) by cytochromeP450 (CYP) .
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochromeP450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .
Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochromeP-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM . Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM) . Kushenol K also inhibits the activity of SGLT1 and SGLT2 .
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochromeP-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochromeP450 (CYP) isoform CYP3A in human liver microsomes.
Hypericin (Standard) is the analytical standard of Hypericin. This product is intended for research and analytical applications. Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP(cytochromeP450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis .
(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the CytochromeP450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth .
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochromeP450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
CYP21A2 Protein, a cytochrome P450 monooxygenase, crucially hydroxylates progesterone and 17alpha-hydroxyprogesterone at C-21, yielding vital intermediates for mineralocorticoid and glucocorticoid biosynthesis in adrenal steroidogenesis. This enzymatic process involves molecular oxygen, with NADPH providing essential electrons via cytochrome P450 reductase (CPR). CYP21A2 plays a pivotal role in regulating adrenal cortex hormone production. CYP21A2 Protein, Human (His) is the recombinant human-derived CYP21A2 protein, expressed by E. coli, with N-6*His labeled tag. The total length of CYP21A2 Protein, Human (His) is 494 a.a., with molecular weight of ~59.9 kDa.
The CYP102A1 protein acts as a fatty acid monooxygenase, catalyzing the hydroxylation of fatty acids at various positions. The protein also exhibits NADPH-dependent reductase activity, promoting electron transfer within its domain. CYP102A1 Protein, Priestia megaterium (P. pastoris, His) is the recombinant CYP102A1 protein, expressed by P. pastoris , with C-6*His labeled tag. The total length of CYP102A1 Protein, Priestia megaterium (P. pastoris, His) is 471 a.a., with molecular weight of 55.2 kDa.
CYP3A4 Protein, a cytochrome P450 monooxygenase, catalyzes diverse substrate metabolism, including sterols, hormones, and fatty acids. Mechanistically, it employs molecular oxygen for hydroxylation, impacting androgen metabolism, cholesterol, and retinoid pathways. Notably, it contributes to drug metabolism and regulates vitamin D catabolism, essential for calcium homeostasis. CYP3A4 Protein, Human (Cell-Free, His) is the recombinant human-derived CYP3A4 protein, expressed by E. coli Cell-free, with N-10*His labeled tag. The total length of CYP3A4 Protein, Human (Cell-Free, His) is 502 a.a., with molecular weight of 63.3 kDa.
CYP11B2 Protein, a cytochrome P450 monooxygenase, synthesizes aldosterone, pivotal for salt and water balance, impacting blood pressure and cardiovascular health. Mechanistically, it orchestrates three oxidative reactions, forming aldosterone, utilizing molecular oxygen and a mitochondrial transfer system. Additionally, CYP11B2 may be involved in the androgen metabolic pathway, expanding its physiological roles. CYP11B2 Protein, Human (His-SUMO) is the recombinant human-derived CYP11B2 protein, expressed by E. coli, with N-6*His, N-SUMO labeled tag. The total length of CYP11B2 Protein, Human (His-SUMO) is 479 a.a., with molecular weight (affected by relative charge) of 66 KDa.
The CYP3A4 protein, encoded by the CYP3A4 gene, is a key enzyme in drug metabolism and the synthesis of cholesterol, steroids, and lipids. It localizes to the endoplasmic reticulum and is induced by glucocorticoids and certain drugs. CYP3A4 Protein, Human (His) is the recombinant human-derived CYP3A4 protein, expressed by E. coli , with N-His labeled tag. The total length of CYP3A4 Protein, Human (His) is 502 a.a., with molecular weight of ~59.2 kDa.
CYP51 Proteinas is a sterol 14α-demethylase that acts with an unknown physiological substrate and accepts electrons from the iron-sulfur ferredoxin Fdx. In vitro, it catalyzes the C14-demethylation of lanosterol, 24,25-dihydrolanosterol, and obtanyol, showing stereoselectivity in producing 8,14-diene. CYP51 Protein, Mycobacterium tuberculosis (Baculovirus, His-Myc) is the recombinant CYP51 protein, expressed by Sf9 insect cells , with N-10*His, C-Myc labeled tag. The total length of CYP51 Protein, Mycobacterium tuberculosis (Baculovirus, His-Myc) is 451 a.a., with molecular weight of ~54.8 kDa.
ERG11 Proteinas is a sterol 14α-demethylase, a key enzyme in the ergosterol biosynthetic pathway, particularly in the late pathway that occurs in the endoplasmic reticulum membrane. ERG11 catalyzes the three-step removal of the 14α-methyl group from lanosterol, releasing it as a formate, resulting in the conversion of the sterol into a key intermediate in ergosterol biosynthesis. ERG11 Protein, Saccharomyces cerevisiae (GST) is the recombinant ERG11 protein, expressed by E. coli , with N-GST labeled tag. The total length of ERG11 Protein, Saccharomyces cerevisiae (GST) is 20 a.a., with molecular weight of ~29.1 kDa.
7-Ethoxycoumarin-d5 is deuterium labeled 7-Ethoxycoumarin. 7-Ethoxycoumarin is a substrate for cytochromeP450(CYP450) and has been used in the functional characterization of various CYPs[1].
Clotrimazole-d5 is the deuterium labeled Clotrimazole. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochromeP450) inhibitor. Clotrimazole has antibacterial activity[1][2].
Clotrimazole-d10 is deuterated labeled Clotrimazole (HY-10882). Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochromeP450) inhibitor. Clotrimazole has antibacterial activity.
Isonicotinic acid-d4 is the deuterium labeled Isonicotinic acid[1]. Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochromeP450 (CYP) enzymes, e.g., CYP2C[2].
Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochromeP-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
2-Naphthol-d8 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochromeP450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
2-Naphthol-d7 is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochromeP450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].
Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochromep450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochromeP450 3A (CYP3A) enzymes[1][2].
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochromeP450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochromeP450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochromeP450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
4-Hydroxyatomoxetine-d3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochromeP450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor[1].
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochromeP450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochromeP450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
4'-Hydroxy diclofenac-d4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochromeP450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[1][2].
Chlorzoxazone-d3 is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochromeP450 2E1 (CYP2E1) activity in humans.
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochromeP450 (CYP) 2C9 and CYP3A[1][2][3].
4'-Hydroxy diclofenac- 13C6 is the 13C labeled 4'-Hydroxy diclofenac[1]. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochromeP450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[2][3].
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochromeP450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochromeP450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
Aromatase Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 58 kDa, targeting to Aromatase. It can be used for WB,IP assays with tag free, in the background of Human, Mouse, Rat.
Cytochrome P450 17A1 Antibody (YA786) is a non-conjugated and Mouse origined monoclonal antibody about 57 kDa, targeting to Cytochrome P450 17A1 (6E1). It can be used for WB assays with tag free, in the background of Human.
CYP11A1 Antibody is an unconjugated, approximately 53/57 kDa, rabbit-derived, anti-CYP11A1 polyclonal antibody. CYP11A1 Antibody can be used for: WB, ELISA, IHC-P, IHC-F, Flow-Cyt, ICC, IF expriments in human, mouse, rat, and predicted: dog, pig, cow, horse, rabbit, sheep background without labeling.
CYP7A1 Antibody is an unconjugated, approximately 55 kDa, rabbit-derived, anti-CYP7A1 polyclonal antibody. CYP7A1 Antibody can be used for: WB, ELISA, IHC-P, IHC-F, ICC, IF, expriments in human, mouse background without labeling.
MS-PPOH is a potent and selective cytochromeP450(CYP)epoxygenase inhibitor . MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 μM, respectively . MS-PPOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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