Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
28 Results for "
Human CYP2D6
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "Human CYP2D6" in MCE Product Catalog:
Cat. No.: HY-169119
Target:
Research Areas:
Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes .
Cat. No.: HY-173032
Target:
Research Areas:
VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
Cat. No.: HY-10672
CAS No.: 1034708-07-0
Research Areas:
Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
Cat. No.: HY-187015
CAS No.: 74141-74-5
Synonyms: NSC 314055
Target:
Research Areas:
SR-2555 (NSC 314055) is a CYP2D6 inhibitor with an IC50 of 1017 μM against human CYP2D6. SR-2555 inhibits the AMMC demethylase activity of recombinant CYP2D6; differentially enhances the sensitivity of hypoxic cells to the lethal effect of γ-rays; and exhibits cytotoxicity against hypoxic cells. SR-2555 can be used in cancer-related research .
Cat. No.: HY-N2129A
CAS No.: 58546-00-2
Target:
Cat. No.: HY-12651D
CAS No.: 57152-56-4
Synonyms: (-)-Primaquine
(R)-Primaquine ((−)-Primaquine) is the R-configured enantiomer of Primaquine (HY-12651A). (R)-Primaquine is an antimalarial agent. The Vmax and Km values of (R)-Primaquine metabolism by recombinant human CYP2D6 are 0.42 μmol/min/mg and 21.6 μM, respectively. (R)-Primaquine can be used in malaria-related research .
Cat. No.: HY-187364
CAS No.: 3050594-88-9
Target:
Research Areas:
TRPV4 antagonist-7 is a potent and selective TRPV4 antagonist with an IC50 of 0.2 nM against human targets. TRPV4 antagonist-7 binds to the voltage-sensor-like domain cavity of TRPV4 and inhibits channel activity through the formation of salt bridges, hydrogen bonds, and edge-to-face π-stacking interactions. TRPV4 antagonist-7 induces phospholipid accumulation in HepG2 C3A cells in vitro with an IC50 of 3.8 μM, and exhibits moderate inhibitory effects on CYP2D6 with an IC50 of 5.1 μM. TRPV4 antagonist-7 dose-dependently inhibits GSK1016790A (HY-19608)-induced bronchoconstriction in rats and cough in guinea pigs. TRPV4 antagonist-7 can be used in studies related to respiratory system diseases .
Cat. No.: HY-18719H
CAS No.: 1032008-71-1
Research Areas:
Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
