Cytochrome P450 Inhibitor

Minamestane (FCE 24928) is a selective and competitive aromatase inhibitor with an IC₅₀ value of 45.7 nM. Minamestane is promising for research of postmenopausal breast cancer.

Quilseconazole (Standard) is the analytical standard of Quilseconazole (HY-109040). This product is intended for research and analytical applications. Quilseconazole (VT-1129) is an orally active, highly selective fungal cytochrome P450 enzyme Cyp51 inhibitor that can cross the blood-brain barrier. Quilseconazole prevents the synthesis of ergosterol, an important component of the fungal cell membrane, by inhibiting Cyp51. Quilseconazole has minimal effects on human CYP enzymes. Quilseconazole has antifungal activity and can be used in the study of cryptococcal meningitis and other diseases.

Uniconazole-P is a potent competitive inhibitor of Arabidopsis CYP707A3 with an IC₅₀ of 68 nM and a K_i of 8.0 nM. Uniconazole-P inhibits ent-kaurene oxidase, blocking gibberellin biosynthesis via reduced ent-kaurene to ent-kaurenoic acid oxidation. Uniconazole-P inhibits plant growth.

Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC₅₀=8.092 μM) over humans (IC₅₀=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans.

DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC₅₀ values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC₅₀ of 18.5 μM, and exhibits stability in mouse plasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia.

Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC₅₀ and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC₅₀ and Ki values of 22.54? μM and 18.02 μM, respectively.

Cloperidone acts as an inhibitor and substrate of CYP2C9, with an IC₅₀ of 17.7 μM. Cloperidone exhibits enhanced cytotoxicity in cells expressing CYP2C9. It can be used in the research of sedative/hypnotic-related diseases.

CYP51-IN-29 (Compound B3) is a CYP51 inhibitor and antifungal agent. CYP51-IN-29 effectively suppresses the yeast-to-hyphal transition. CYP51-IN-29 exhibits potent antifungal activity against Candida albicans.

Acanthoic acid (NP1302) is an orally active pimarane-type diterpenoid. Acanthoic acid is isolated from the root bark of Araliaceae family plant Eleutherococcus senticosus (Siberian ginseng). Acanthoic acid activates LXR and FXR. Acanthoic acid activates the AMPK-LKB1, SIRT1, and p38 MAPK signaling pathways and increases the phosphorylation level of ACC. Acanthoic acid downregulates the expression of SREBP-1, CYP2E1, HIF-1α, and PPARγ, and upregulates the expression of PPARα. Acanthoic acid induces Apoptosis by activating Caspase-3, promoting PARP cleavage, and downregulating Bcl-xL. Acanthoic acid exhibits antioxidant, anti-fibrotic, and hepatoprotective effects. It reduces lipid accumulation and lipogenesis. Acanthoic acid is used in studies on non-alcoholic fatty liver disease, alcoholic liver disease, acute promyelocytic leukemia, and Acetaminophen-induced hepatotoxicity.

Verapamil-d₃ ((±)-Verapamil-d₃) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.

4-CPI (4-(4-Chlorophenyl)imidazole) is a CYP2B4 inhibitor with an IC₅₀ of 0.11 μM and a K_d of 0.043 μM. The K_s of 4-CPI for cytochrome P450eryF (S93C/C154S mutant) is 9.4 μM, with no allosteric cooperative effect of ligand binding. 4-CPI binds to CYP2B4 at a 1:1 ratio, which induces substantial conformational changes in the enzyme's active pocket to form a closed crystal conformation (PDB:1SUO). 4-CPI can be used to investigate the flexibility of P450 active pockets, protein-ligand binding thermodynamics, and the allosteric mechanisms of P450.

Cephaeline (dihydrochloride) (Standard) is the analytical standard of Cephaeline (dihydrochloride). This product is intended for research and analytical applications. Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.

CYP51-IN-31 (compound T24) is a selective CYP51 inhibitor with potent and broad-spectrum antifungal activity, including efficacy against drug-resistant fungal strains. CYP51-IN-31 exhibits fungicidal activity against Candida parapsilosis, anti-biofilm activity, and the ability to inhibit fungal morphological transitions. CYP51-IN-31 can be used for infection research.

Democonazole is an imidazole antifungal agent that blocks ergosterol synthesis by inhibiting CYP450 14α-lanosterol demethylase (CYP51), thereby disrupting the integrity and fluidity of fungal cell membranes. Democonazole is lipophilic, which enhances its ability to penetrate fungal cell membranes and inhibit ergosterol synthesis. Democonazole can be used in studies related to fungal infections.

CYP51-IN-32 is an antifungal agent with an IC₅₀ of 0.331 μM against CYP51 of Candida albicans. CYP51-IN-32 releases hydrogen sulfide (H₂S) and inhibits hyphal formation and biofilm development of Candida albicans. CYP51-IN-32 can be formulated into PEG-based nanovesicles. CYP51-IN-32 is applicable to the research of Candida albicans infection.

Terbufibrol (Standard) is the analytical standard of Terbufibrol (HY-101812). This product is intended for research and analytical applications. Terbufibrol is an orally active lipid-lowering agent. Terbufibrol inhibits hepatic Cholesterol 7 alpha-hydroxylase. Terbufibrol blocks a step between Acetate and HMG-CoA in the hepatic cholesterol synthesis process. Terbufibrol reduces serum total cholesterol, HDL, LDL, lipoprotein levels, and the cholesterol/phospholipid ratio, with dose- and sex-dependent changes in lipoprotein components. Terbufibrol exerts sustained cholesterol-lowering activity in baboons and rats. Terbufibrol can be used in research related to hypercholesterolemia.

Chlorpromazine (Standard) is the analytical standard of Chlorpromazine (HY-12708). This product is intended for research and analytical applications. Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT_2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNa_v1.7 channels (IC₅₀=25.9 μM; concentration-dependent) and HERG potassium channels (IC₅₀=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis.

6α-Fluorotestosterone is a non-aromatizable aromatase inhibitor, with IC₅₀ values of 115 nM and 580 nM against human and rat aromatase, respectively. 6α-Fluorotestosterone binds to the substrate site of human aromatase P450arom with a K_i of 150 nM, but is not aromatized into estrogen. In vivo, 6α-Fluorotestosterone maintains sexual behavior in castrated male rats (with an effect comparable to that of testosterone), induces defeminization of sexual development, and inhibits nuclear translocation of hypothalamic estrogen receptors; its pro-mating effect is blocked by the aromatase inhibitors ATD and Fadrozole (HY-14247A). Combined with Progesterone (HY-N0437), 6α-Fluorotestosterone induces lordosis behavior in ovariectomized female rats. 6α-Fluorotestosterone can be used in studies related to anovulatory infertility and sexual behavior regulation.

CYP51-IN-28 (compound B9) is a CYP51 inhibitor. CYP51-IN-28 is an efficient, broad-spectrum, and low toxicity antifungal molecule. CYP51-IN-28 can be used for research on fungal infections.

CYP51/Hsp90-IN-1 (Compound MM4) is a dual CYP51/Hsp90 inhibitor. CYP51/Hsp90-IN-1 shows antifungal activity against Candida albicans and effectively inhibits important fungal virulence factors. CYP51/Hsp90-IN-1 is promising for research of invasive candidiasis.