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
122 Results for "
human microsomes
" in MedChemExpress (MCE) Product Catalog:
Products (122)
122 Results for "human microsomes" in MCE Product Catalog:
Cat. No.: HY-W015912S
Synonyms: 2-Furyl methyl ketone-d3
Cat. No.: HY-158316
CAS No.: 2758569-43-4
Target:
Research Areas:
BTL-MK (Compound 19) an orally active antiallergic agent, that inhibits degranulation of mast cells with an IC50 of 6.7 μM, through binding to the inhibitory receptor FcγRIIB. BTL-MK improves the metaboilic stability in human liver microsomes. BTL-MK ameliorates the allergic response in Ovalbumin, low endotoxin (HY-W250978A)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
Target:
Cat. No.: HY-101284A
CAS No.: 1031063-36-1
Target:
Research Areas:
(E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity .
Cat. No.: HY-124626
CAS No.: 147780-50-5
Target:
Research Areas:
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .
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-139722
CAS No.: 2611373-74-9
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo. Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-182255
CAS No.: 217187-87-6
Target:
Research Areas:
ED-594 is the glucuronide form of NB-506. ED-594 is one of the major metabolites of NB-506 in rat bile, mouse liver microsomes, rat liver microsomes and human liver microsomes .
Category:
Target:
Cat. No.: HY-179369
CAS No.: 1379213-90-7
Synonyms: 4-HTP
Target:
Research Areas:
Cat. No.: HY-171185
CAS No.: 368454-88-0
Target:
Research Areas:
CP-611,781 is a diol metabolite of ezlopitant alkene (CJ-12,458). In human liver microsomes, the apparent KM value of 5.4 μM for the formation of CP-611,781 .
Cat. No.: HY-W716241
CAS No.: 71525-06-9
Target:
Research Areas:
3',4'-Dihydroxytrimethoprim is a Trimethoprim (HY-B0510) derivative. 3',4'-Dihydroxytrimethoprim forms via sequential O-demethylation of Trimethoprim in human liver microsomes. 3',4'-Dihydroxytrimethoprim can be used for metabolic research .
Cat. No.: HY-114572
CAS No.: 1635405-90-1
Target:
Research Areas:
1D-2 is a c-Met protein kinase inhibitor, with a human-derived IC50 of 1.45 nM. 1D-2 inhibits the proliferation of cancer cells and exhibits metabolic stability in human and rat liver microsomes. 1D-2 can be used in related research on non-small cell lung cancer .
Cat. No.: HY-184246
CAS No.: 2791469-19-5
Target:
Research Areas:
SR-34831 is a NAMPT activator, NAD level stabilizer and neuroprotective agent. SR-34831 enhances the enzymatic activity of human NAMPT, prevents intracellular NAD depletion, and counteracts neuronal death induced by toxic misfolded prion proteins. SR-34831 exhibits metabolic stability in human liver microsomes and can be used for the research of protein misfolding neurodegenerative diseases .
Cat. No.: HY-187125
CAS No.: 946400-19-7
11β-HSD1-IN-27 is a human and mouse 11β-hydroxysteroid dehydrogenase type I inhibitor. 11β-HSD1-IN-27 inhibits catalytic activity of target enzymes in cell-based assays. 11β-HSD1-IN-27 exhibits moderate stability in mouse and human liver microsomes .
Cat. No.: HY-N19921
CAS No.: 144608-09-3
Target:
Cat. No.: HY-184381
Target:
Research Areas:
PBC21 is an orally active, brain-penetrant, highly selective, mixed-type reversible MAO-B inhibitor (IC50 = 14 nM, SI for MAO-A > 2857). PBC21 exhibits no significant cytotoxicity across various human cell lines and demonstrates good metabolic stability in rat and human liver microsomes. In an MPTP (HY-W114750)-induced rat model of Parkinson's disease, PBC21 exhibits significantly improving motor function and positioning itself as a promising candidate for Parkinson's disease research .
Cat. No.: HY-B0476S3
CAS No.: 286425-41-0
Synonyms: Acetophenetidin-13C-1
Cat. No.: HY-181917
Target:
Research Areas:
Pantothenate kinase-IN-3 is an orally active PANK3-selective binder and CoA biosynthesis activator with a human PANK3 Ki of 9.1 nM, human PANK3 Ka of 1.8 nM, human PANK1β Ki of 113 nM, human PANK1β Ka of 23.4 nM, and oral effectiveness.Pantothenate kinase-IN-3 binds PANK3 via a water-mediated interaction between its sulfonamide NH and Gly193, elevates cellular, hepatic, and forebrain CoA levels, and shows improved metabolic stability in mouse and human microsomes.Pantothenate kinase-IN-3 has solubility properties favorable at pH 7.Pantothenate kinase-IN-3 can be used for the research of hepatic metabolic CoA deficiencies (acidemias) .
Cat. No.: HY-125505A
CAS No.: 864295-20-5
Research Areas:
BI-11634 free base is an orally active factor Xa inhibitor and a CYP3A4 substrate. The apparent Km values for BI-11634 free base metabolism are 23 μM in human liver microsomes (HLMs) and 7.6 μM with recombinant CYP3A4. BI-11634 free base can be used for thromboembolic disease and CYP3A4-mediated drug metabolism research .
-
-
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
