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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
20 Results for "
human and rat liver microsomes
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "human and rat liver microsomes" in MCE Product Catalog:
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Research Areas:
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
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1 Cited Publications
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Cardiovascular Disease Metabolic Disease Inflammation/Immunology
MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
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CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes .
Cat. No.: HY-N4031
CAS No.: 82375-29-9
Cat. No.: HY-173084
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BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes .
Cat. No.: HY-172147
CAS No.: 2761347-44-6
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SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
Cat. No.: HY-10864R
CAS No.: 546141-08-6
Synonyms: KDS-4103 (Standard)
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URB-597 (Standard) is the analytical standard of URB-597. This product is intended for research and analytical applications. URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
Cat. No.: HY-146410
CAS No.: 2709031-17-2
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AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
Cat. No.: HY-113777
CAS No.: 90780-46-4
Synonyms: 22-Hydroxy Docosahexaenoic acid; 22-OH DHA
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22-HDHA (22-Hydroxy Docosahexaenoic acid) is an oxidation product of docosahexaenoic acid. In vitro, it is formed upon incubation of rat liver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
Cat. No.: HY-157931
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Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
Cat. No.: HY-171462
CAS No.: 2133010-38-3
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SMW139 is a selective allosteric antagonist of P2X7 receptor, with a Ki value of 32 nM for human P2X7R. The half-life of SMW139 in rat liver microsomes is 47 minutes. SMW139 can be used for inflammation, Alzheimer’s disease, multiple sclerosis study .
Cat. No.: HY-149481
CAS No.: 2826198-44-9
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D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders .
Cat. No.: HY-123639
CAS No.: 261766-32-9
Synonyms: N-(2-Phenylethyl)-indomethacin amide
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LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively .
Cat. No.: HY-173024
CAS No.: 3053390-98-7
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TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
Cat. No.: HY-155051
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Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .
Cat. No.: HY-182255
CAS No.: 217187-87-6
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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 .
Cat. No.: HY-114572
CAS No.: 1635405-90-1
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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-N19921
CAS No.: 144608-09-3
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Cat. No.: HY-184381
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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-181710
LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer .
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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
