Cytochrome P450 Modulator

Cytochrome P450 Modulators (21):

Cat. No.	Product Name	Effect	Purity

HY-B1462

Chlorzoxazone	Modulator	99.77%
Chlorzoxazone is a SK-type potassium channel activator. Chlorzoxazone modulates FOXO3 phosphorylation and Aβ. Chlorzoxazone enhances immunosuppression, attenuates vasoconstriction, attenuates cognitive deficits, and improves experimental autoimmune encephalomyelitis.

HY-164793

TGFBR1-IN-2	Modulator
TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis.

HY-B0854

Mancozeb	Modulator
Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells.

HY-B1462R

Chlorzoxazone (Standard)	Modulator
Chlorzoxazone (Standard) is the analytical standard of Chlorzoxazone. This product is intended for research and analytical applications.

HY-B1462S

Chlorzoxazone-d₃	Modulator	99.88%
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 cytochrome P450 2E1 (CYP2E1) activity in humans.

HY-135331

N-Desmethyl-Apalutamide	Modulator	99.68%
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.

HY-173033

MI-883	Modulator
MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC₅₀=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC₅₀=0.1 μM). MI-883 stimulates CAR LBD assembly (EC₅₀=0.38 µM) and CAR3 variant activation (EC₅₀=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC₅₀=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models.

HY-Z2667

(R)-Esomeprazole	Modulator
(R)-Esomeprazole ((R)-Omeprazole; (+)-Omeprazole) is an orally active cytochrome P450 2C19, CYP3A4, and CYP2C9-related metabolic modulator. (R)-Esomeprazole can be used in studies of digestive system diseases and compound metabolic interactions.

HY-W700800

Flu-6	Modulator	98.44%
Flu-6 is a metabolite of Flutamide (HY-B0022). FLU-6 production in the liver requires the involvement of NADPH: cytochrome P450 reductase (CPR). Flutamide can inhibit prostate cancer progression.

HY-W010253

Benzylurea	Modulator	99.94%
Benzylurea is an anti-inflammatory agent. Benzylurea inhibits LPS (HY-D1056)-induced upregulation of MTCH2 expression and regulates pathways associated with mitochondrial function, inflammation and cell survival. Benzylurea alleviates LPS-induced proliferation inhibition and apoptosis of periodontal ligament fibroblasts, as well as the release of proinflammatory cytokines. Benzylurea can be used in studies related to periodontitis.

HY-181629A

ZSTK3744 hydrochloride	Modulator
ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

HY-181629

ZSTK3744	Modulator
ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

HY-118216

Bitertanol	Modulator	98.70%
Bitertanol (Biloxazol) is a potent antifungal agent. Bitertanol also is an CYP1A1, CYP2B, and CYP3A inducer in vivo and an CYP1A inhibitor in vitro.

HY-182284

Anticancer agent 310	Modulator
Anticancer agent 310 is an antitumor agent. Anticancer agent 310 releases nitric oxide to induce mitochondrial ROS burst, triggers mitochondrial dysfunction and activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 apoptotic pathway. Anticancer agent 310 also reduces the levels of SHMT2 and MTHFD2, decreases the ratios of NADPH/NADP⁺ and GSH/GSSG, thereby disrupting redox homeostasis and exacerbating intracellular ROS accumulation. Anticancer agent 310 can be used in research related to gastric cancer.

HY-13762

Tesmilifene	Modulator
Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance.

HY-135331S

N-Desmethyl-Apalutamide-¹⁵N,d₄	Modulator
N-Desmethyl-Apalutamide-15N,d4 is the ¹⁵N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.

HY-133078

Thienyldecyl Isothiocyanate	Modulator
Thienyldecyl isothiocyanate is an analog of thienylbutyl isothiocyanate that, like many isothiocyanates, demonstrates antiproliferative activity against cancer cells presumably by modulation of xenobiotic-metabolizing enzymes, such as by inhibition of cytochrome P450, and/or by induction of phase II detoxifying enzymes.

HY-13762S

Tesmilifene-d₄	Modulator
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance.

HY-B1462S2

Chlorzoxazone-¹³C,¹⁵N,d₂	Modulator
Chlorzoxazone-¹³C,¹⁵N,d₂ is ¹³C-, ¹⁵N-, and deuterium-labeled Chlorzoxazone (HY-B1462).

HY-163804

Cyprocide-B	Modulator
Cyprocide-B is activated by Cytochrome P450 and converted to electrophilic metabolites that selectively kill nematodes C. elegans. Cyprocide-B is promising for research of selective nematicide.

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