Search Result
Results for "
liver microsomes
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-16718
-
|
PF-00251802
|
Glucocorticoid Receptor
Cytochrome P450
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Inflammation/Immunology
Endocrinology
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Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
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-
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- HY-16718A
-
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PF-00251802 hydrochloride
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Glucocorticoid Receptor
Cytochrome P450
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Inflammation/Immunology
Endocrinology
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Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
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-
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- HY-N8094
-
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Cytochrome P450
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Others
|
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Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
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-
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- HY-149395
-
|
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Bacterial
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Infection
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MmpL3-IN-3 (Compound 12) is a MmpL3 inhibitor. MmpL3-IN-3 shows a MIC of 0.1 μM against H37Rv. MmpL3-IN-3 shows good stability in mouse liver microsomes. MmpL3-IN-3 can be used for anti-tubercular research .
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-
-
- HY-157931
-
|
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Histamine Receptor
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Neurological Disease
|
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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 .
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-
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- HY-N5132
-
|
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Others
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Others
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(-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .
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-
-
- HY-150578
-
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Keap1-Nrf2
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Inflammation/Immunology
|
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Keap1-Nrf2-IN-12 is a potent Keap1-Nrf2 inhibitor with an IC50 value of 2.30 µM. Keap1-Nrf2-IN-12 shows metabolic stability in human liver microsomes .
|
-
-
- HY-10864
-
URB-597
4 Publications Verification
KDS-4103
|
FAAH
Autophagy
Mitophagy
|
Neurological Disease
|
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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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-
-
- HY-17614
-
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SMT C1100; BMN 195; VOX-C1100
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Cytochrome P450
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Others
|
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Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
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-
-
- HY-155141
-
|
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Cytochrome P450
|
Cancer
|
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hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
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-
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- HY-155051
-
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Apoptosis
Histone Methyltransferase
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Cancer
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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 .
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-
- HY-155050
-
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Apoptosis
Histone Methyltransferase
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Cancer
|
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PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
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- HY-123370
-
|
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Proton Pump
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Metabolic Disease
Cancer
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FR-167356 is a potent, orally active and selective vacuolar ATPase inhibitor with IC50 values of 170, 220, 370, and 1200 nM for osteoclast plasma membranes, macrophage microsomes, renal brush border membranes, and liver lysosomal membranes, respectively. FR-167356 inhibits bone resorption and ovariectomy-induced bone loss .
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- HY-146410
-
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Angiotensin Receptor
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Others
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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 .
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-
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- HY-112690A
-
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Remofovir mesylate
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Cytochrome P450
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Metabolic Disease
|
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Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
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- HY-101627
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- HY-N6739
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-
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- HY-N6702
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-
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- HY-163291
-
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Bacterial
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Infection
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AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
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-
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- HY-126665
-
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ADC Cytotoxin
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Cancer
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DMEA-PNU-159682 (molecule D12) is a ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682 .
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- HY-N4070
-
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Others
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Others
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6"-O-Acetylgenistin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetylgenistin significantly inhibits lipid peroxidation in rat liver microsome with an IC50 of 10.6 μM .
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- HY-N4071
-
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Others
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Others
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6"-O-Acetyldaidzin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetyldaidzin significantly inhibits lipid peroxidation in rat liver microsome with an IC50 of 8.2 μM .
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- HY-126665A
-
|
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ADC Cytotoxin
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Cancer
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DMEA-PNU-159682 (molecule D12) dichloroacetate is an ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682 .
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- HY-B0794S
-
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EGFR
IGF-1R
Drug Metabolite
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Others
|
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AZ7550-d5 is the deuterium labeled AZ7550 (HY-B0794). AZ7550, an active metabolite of Osimtinib (AZD9291; HY-15772), inhibits the activity of IGF1R with an IC50 of 1.6 μM[1][2].
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-
-
- HY-U00369
-
|
|
Acyltransferase
|
Cardiovascular Disease
|
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FCE 28654 is an inhibitor of acylCoA: cholesterol acyltransferase (ACAT), weakly inhibiting ACAT in microsomes from rabbit aorta and intestine, and monkey liver, with IC50s of 2.55, 1.08 and 5.69 μM, respcetively.
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-
- HY-100432
-
LOC14
2 Publications Verification
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|
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LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
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-
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- HY-B0476
-
|
Acetophenetidin
|
COX
|
Inflammation/Immunology
|
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Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
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- HY-125568
-
|
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Others
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Others
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Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in rat liver microsomes free from vitamin E .
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- HY-N11676
-
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Drug Metabolite
|
Cancer
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6-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .
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- HY-N11677
-
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Drug Metabolite
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Others
|
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7-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .
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- HY-N1483
-
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Potassium Channel
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Cardiovascular Disease
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Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
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-
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- HY-129105
-
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GABA Receptor
Cytochrome P450
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Neurological Disease
|
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Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
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- HY-100644
-
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Trimethoprim 1-N-oxide
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Trimethoprim N-oxide (Trimethoprim 1-N-oxide) belongs to human urinary metabolites. Trimethoprim N-oxide is generated by oxidation of nitrogen atoms in the pyrimidine ring. Trimethoprim N-oxide is formed predominantly by CYP1A2 in human liver microsomes .
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- HY-153822
-
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Tau Protein
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Neurological Disease
|
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JG-23 is a 4-chloro modified analog with ability to promote t-tau degradation. JG-23 exhibits good metabolic stability with a long T1/2 value (36 min) in mouse liver microsome assays .
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- HY-146111
-
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IRAK
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Cancer
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IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg .
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- HY-N3806
-
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Acyltransferase
ERK
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Infection
Cardiovascular Disease
Cancer
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Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
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- HY-139721
-
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HIV
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Infection
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Tenofovir-C3-O-C15-CF3 (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.
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- HY-151957
-
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Bacterial
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Infection
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Antitubercular agent 34 (compound 42g) is an antitubercular agent. Antitubercular agent 34 inhibits the growth of MtbH37Rv with a MIC90 value of 1.25 μg/mL with the ability of escaping metabolic degradation by human liver microsomes. Antitubercular agent 34 can be used for the research of tuberculosis .
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- HY-B0476S
-
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Acetophenetidin-d5
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COX
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Inflammation/Immunology
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Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
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- HY-B0476S1
-
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COX
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Inflammation/Immunology
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Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
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- HY-B0476R
-
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Acetophenetidin (Standard)
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COX
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Inflammation/Immunology
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Phenacetin (Standard) is the analytical standard of Phenacetin. This product is intended for research and analytical applications. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
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- HY-149481
-
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Dopamine Receptor
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Neurological Disease
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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 .
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- HY-156093
-
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Tryptophan Hydroxylase
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Metabolic Disease
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TPH1-IN-1 (compound 40) is a xanthine derivative and an inhibitor of tryptophan hydroxylase TPH1 (IC50: 110.1 nM). TPH1-IN-1 has good in vitro activity and liver microsome stability, and effectively inhibits adipocyte differentiation of T3-L1 cells .
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- HY-15796
-
GNE0877
2 Publications Verification
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LRRK2
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Neurological Disease
|
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GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience .
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-
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- HY-120608
-
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MCHR1 (GPR24)
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Metabolic Disease
|
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BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities .
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-
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- HY-N6704
-
|
|
ERK
Apoptosis
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Cancer
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Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes .
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-
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- HY-143326
-
|
|
Bacterial
|
Infection
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Antibacterial agent 83 (compound 17h) displays potent antibacterial activity against various vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). Antibacterial agent 83 can significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. Antibacterial agent 83 is metabolically stable in human liver microsomes .
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- HY-162408
-
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Protease Activated Receptor (PAR)
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Others
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PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min .
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- HY-162409
-
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Protease Activated Receptor (PAR)
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Others
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PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min .
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- HY-163032
-
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FABP
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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FABP4-IN-3 (compound C3) is a highly selective FABP4 inhibitor (FABP4 Ki = 25 ± 3 a nM, FABP3 Ki = 15.03 μM) which exhibits a 601-fold selectivity over FABP3. FABP4-IN-3 also shows metabolic stability and potent cellular anti-inflammatory activity, making it promising to get involved in the research of metabolic disease, cardiac dysfunction and inflammation-related disease .
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- HY-152118
-
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Cytochrome P450
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Cancer
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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 .
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- HY-107460
-
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Ephrin Receptor
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Cancer
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LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC .
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- HY-143255
-
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Phosphodiesterase (PDE)
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Cancer
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Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
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- HY-149920
-
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Microtubule/Tubulin
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Cancer
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Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
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- HY-155111
-
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Phospholipase
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Neurological Disease
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nSMase2-IN-1 is an orally active Neutral sphingomyelinase 2 (nSMase2) inhibitor with an IC50 value of 0.13 ± 0.06 μM. nSMase2-IN-1 is metabolically stable in liver microsomes and orally available with a favorable brain-to-plasma ratio. nSMase2-IN-1 can be used for nervous system disease research .
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- HY-162121
-
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Others
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Cancer
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Antitumor agent-129 (Compound 68) is a thiazolidin-4-one sulfone derivative and an Osteosarcoma (OS) inhibitor with an IC50 value of 0.217 μM, a half-life of 73.8 min (mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115%, intraperitoneal administration). Antitumor agent-129 is a potential candidate for OS research .
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- HY-148060
-
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JAK
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Cancer
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JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively .
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- HY-N0904
-
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Ginsenoside compound K; Ginsenoside K
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COX
NO Synthase
Cytochrome P450
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Inflammation/Immunology
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Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
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- HY-126687
-
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Drug-Linker Conjugates for ADC
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Cancer
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Mal-PEG4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker Mal-PEG4-VC-PAB and a potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 includes metabolites of nemorubicin (MMDX) from liver microsomes and ADC cytotoxin PNU-159682 .
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- HY-151958
-
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Bacterial
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Infection
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Antitubercular agent-35 (compound 42l) is an antitubercular agent. Antitubercular agent-35 inhibits the growth of MtbH37Rv and M. Marinum with MIC90 values of 1.25 and 2 μg/mL, respectively. Antitubercular agent-35 shows the ability of escaping metabolic degradation by human liver microsomes. Antitubercular agent-35 can be used for the research of tuberculosis .
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- HY-156672
-
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FGFR
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Cancer
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S6K2-IN-1 (Compound 2) is a S6K2 inhibitor (IC50: 22 nM). S6K2-IN-1 also inhibits FGFR4 (IC50: 216 nM). S6K2-IN-1 has acceptable stability in mouse liver microsomes .
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- HY-162238
-
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Parasite
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Infection
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OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .
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- HY-126689
-
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Drug-Linker Conjugates for ADC
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Cancer
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Mal-Phe-C4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker Mal-Phe-C4-VC-PAB and a potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 includes metabolites of nemorubicin (MMDX) from liver microsomes and ADC cytotoxin PNU-159682 .
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- HY-147754
-
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Btk
JAK
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Inflammation/Immunology
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JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research .
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- HY-150508
-
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CD38
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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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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- HY-N7454
-
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Antibiotic
Bacterial
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Infection
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Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
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- HY-146594
-
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM) .
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-
- HY-136582
-
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Androgen receptor-IN-2
|
Androgen Receptor
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Cancer
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Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumor activity against prostate cancer .
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- HY-N3807
-
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Acyltransferase
ERK
NF-κB
|
Infection
Cardiovascular Disease
Cancer
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Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes . Enniatin B1 crosss the blood-brain barrier . Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation .
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-
- HY-153394
-
|
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Fungal
|
Infection
|
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Aflatoxin Q1 is a hydroxy metabolite of Aflatoxin B1 (AFB1), which is a mycotoxin produced by Aspergillus flavus (A. flavus). Aflatoxin Q1, as well as and aflatoxin B1 8,9-oxide, is the major oxidative products formed from aflatoxin B1 in human liver microsomes, at all substrate concentrations. the 3 alpha-hydroxylation of aflatoxin B1 to aflatoxin Q1 is a potentially significant detoxication pathway .
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-
- HY-123639
-
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N-(2-Phenylethyl)-indomethacin amide
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COX
|
Inflammation/Immunology
Cancer
|
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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 .
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- HY-157325
-
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RIP kinase
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Inflammation/Immunology
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RIPK2-IN-5 (compound 14) is a high affinity and excellent selectivity RIPK2 inhibitor with an IC50 value of 5.1nM. RIPK2-IN-5 has cellular anti-inflammatory effect and can reduce the secretion of MDP-induced TNF-α with a dose-dependent manner. RIPK2-IN-5 shows moderate stability in human liver microsome. RIPK2-IN-5 can be used for the research of immune diseases .
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- HY-N0904R
-
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Ginsenoside compound K(Standard); Ginsenoside K (Standard)
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COX
NO Synthase
Cytochrome P450
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Inflammation/Immunology
|
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Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
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- HY-139722
-
|
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HIV
|
Infection
|
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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.
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- HY-146486
-
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P2Y Receptor
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Inflammation/Immunology
|
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P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes .
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- HY-147907
-
|
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Adenosine Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
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Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .
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-
- HY-107534
-
|
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GnRH Receptor
|
Endocrinology
|
|
AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone .
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-
- HY-126691
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
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DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker DBCO-PEG4-VC-PAB and a potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 includes metabolites of nemorubicin (MMDX) from liver microsomes and ADC cytotoxin PNU-159682. DBCO-PEG4-VC-PAB-DMEA-PNU-159682 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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-
- HY-B0822S1
-
|
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GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
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Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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-
- HY-144123
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0476S
-
|
|
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Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
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-
-
- HY-B0794S
-
|
|
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AZ7550-d5 is the deuterium labeled AZ7550 (HY-B0794). AZ7550, an active metabolite of Osimtinib (AZD9291; HY-15772), inhibits the activity of IGF1R with an IC50 of 1.6 μM[1][2].
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-
-
- HY-B0476S1
-
|
|
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Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
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-
-
- HY-B0822S1
-
|
|
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-126691
-
|
|
|
DBCO
|
|
DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker DBCO-PEG4-VC-PAB and a potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 includes metabolites of nemorubicin (MMDX) from liver microsomes and ADC cytotoxin PNU-159682. DBCO-PEG4-VC-PAB-DMEA-PNU-159682 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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