Cytochrome P450 Inhibitor

Stiripentol (Standard) is the analytical standard of Stiripentol (HY-103392). This product is intended for research and analytical applications. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with K_i of 1.59±0.07 and 0.516±0.065 μM and IC₅₀ of 1.58 and 3.29 μM, respectively.

YM511 (Standard) is the analytical standard of YM511 (HY-105184). This product is intended for research and analytical applications. YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC₅₀s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones.

1-Aminobenzotriazole (Standard) is the analytical standard of 1-Aminobenzotriazole. This product is intended for research and analytical applications. 1-Aminobenzotriazole is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).

2-Nonylimidazole is a CYP2A13 inhibitor with an IC₅₀ of 277 μM. 2-Nonylimidazole modulates the enzymatic activity of CYP2A13. 2-Nonylimidazole is applicable to research on drug metabolism and tobacco-related cancers.

Bergapten (Standard) is the analytical standard of Bergapten. This product is intended for research and analytical applications. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.

Uniconazole (Standard) is the analytical standard of Uniconazole. This product is intended for research and analytical applications. Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC₅₀ of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a Ki of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent.

(R,R)-Voriconazole ((R,R)-UK-109496) is an enantiomer of Voriconazole (HY-76200). Voriconazole (UK-109496) is a second-generation broad-spectrum triazole antifungal compound that inhibits the biosynthesis of fungal ergosterol. Voriconazole exerts its antifungal activity by inhibiting the 14-α-lanosterol demethylation mediated by fungal cytochrome P450 enzymes. Voriconazole exhibits blood-brain barrier permeability.

Eptifibatide (acetate) (Standard) is the analytical standard of Eptifibatide (acetate). This product is intended for research and analytical applications. Eptifibatide acetate is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity.

4-Phenyl-1,2,3-thiadiazole is an CYP2B4 and CYP2E1 inhibitor. 4-Phenyl-1,2,3-thiadiazole inhibits the oxidation of 1-phenylethanol to acetophenone by CYP2B4 and CYP2E1.

(S)-6-O-Desmethylnaproxen (Standard) is the analytical standard of (S)-6-O-Desmethylnaproxen. This product is intended for research and analytical applications. (S)-6-O-Desmethylnaproxen ((S)-6-Desmethyl Naproxen) is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (+)-naproxen ((S)-naproxen). (S)-6-O-Desmethylnaproxen is formed from (S)-naproxen by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2C9.

Curcumenol (Standard) ((+)-Curcumenol (Standard)) is the analytical standard of Curcumenol (HY-N2259). This product is intended for research and analytical applications. Curcumenol ((+)-Curcumenol) is a natural compound with oral efficacy, exhibiting an IC₅₀ of 12.6 μM and a K_i of 10.8 μM against human CYP3A4. Curcumenol inhibits TNFα-induced phosphorylation/degradation of IκBα, phosphorylation/nuclear translocation of NF-κB p65, as well as the upregulation of MMP3, MMP9, MMP13, TRAF3, IL1RL1, TNFα and IL-1β. Curcumenol suppresses LPS-induced phosphorylation of Akt and p38 MAPK, as well as the production of pro-inflammatory mediators/proteins, and downregulates the SLC7A11/NF-κB/TGF-β pathway. Curcumenol binds to and inhibits the activation of Fyn and Lyn, blocks the function of downstream FcεRI signaling components, and reduces the release of allergic mediators/cytokines. Curcumenol upregulates the expression of KDM6B, and promotes chondrocyte proliferation and cartilage repair. Curcumenol induces ferroptosis and apoptosis, regulates the EMT process, and inhibits tumor growth and metastasis of triple-negative breast cancer. Curcumenol possesses anti-inflammatory, neuroprotective, antioxidant, antitumor, antiviral and hepatoprotective activities. Curcumenol can be used in research related to intervertebral disc degeneration, cancer, inflammation, central nervous system neurodegenerative diseases, allergic reactions and knee osteoarthritis.

CYP4Z1-IN-2 (compound 7) is a reversible inhibitor of CYP4Z1 (K_i=2.2 μM), which inhibits the production of 14,15-EET in breast cancer cells. CYP4Z1-IN-2 inhibits the CYP4Z1-mediated Luc-BE O-debenzylation reaction with an IC₅₀ of 5.9 μM.

RPR203494 is a potent inhibitor against CYP isozymes. RPR203494 shows inhibition against p38 kinase with an IC₅₀ value of 9 nM and an EC₅₀ value of 60 nM. RPR203494 demonstrates an inhibition of hepatic Cytochrome P450. RPR203494 is promising for research of rheumatoid arthritis (RA).

Ketoconazole carbonyl-¹³C (Ketoconazol-¹³C) is ¹³C labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

Liarozole (Standard) is the analytical standard of Liarozole. This product is intended for research and analytical applications. Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.

CYP51-IN-30 is a CYP51 inhibitor and fungicidal agent. CYP51-IN-30 inhibits CYP51 activity. CYP51-IN-30 displays potent fungicidal activity with an EC₅₀ value of 2.97 mg/L against S. sclerotiorum.

7-Methoxyflavone (Standard) is the analytical standard of 7-Methoxyflavone (HY-N8487). This product is intended for research and analytical applications. 7-Methoxyflavone is a flavonoid compound that can be isolated from Zornia brasiliensis. 7-Methoxyflavone can bind to human serum albumin and is an aromatase inhibitor. 7-Methoxyflavone has peripheral analgesic and certain antitumor activities. 7-Methoxyflavone is effective against chemical pain but has no significant effect on thermal pain.

Cimicoxib (Standard) is the analytical standard of Cimicoxib. This product is intended for research and analytical applications. Cimicoxib (UR-8880) is an orally active, blood-brain barrier-permeable COX-2 inhibitor that also exerts targeted inhibition on CYP2D15. It has an IC₅₀ of 66 nM against hCOX-2, an IC₅₀ of 1.6 μM against canine CYP2D15, and an IC₅₀ of 0.056 μM against feline CYP2D15. By inhibiting the COX-2 pathway to reduce the production of thromboxane B2 and prostaglandin E2, Cimicoxib exerts antipyretic, anti-inflammatory and analgesic effects. Cimicoxib is metabolized by CYP2D15 to form demethyl-cimicoxib, undergoes glucuronidation via UDP-glucuronosyltransferases, and exhibits biphasic elimination kinetics in beagle dogs. Cimicoxib is widely used in studies of inflammatory diseases, osteoarthritis, and perioperative pain associated with orthopedic or soft tissue surgeries.