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Results for "

Human liver microsomes

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Angiotensin Receptor (1) Antibiotic (1) Apoptosis (2) Autophagy (1) Bacterial (4) Btk (1) CD38 (1) COX (7) Cytochrome P450 (10) Dopamine Receptor (1) Drug Metabolite (3) EGFR (1) FAAH (1) FABP (1) Fungal (1) GABA Receptor (1) Glucocorticoid Receptor (2) Histamine Receptor (1) Histone Methyltransferase (2) HIV (2) IGF-1R (1) IRAK (1) JAK (1) Keap1-Nrf2 (1) Microtubule/Tubulin (1) Mitophagy (1) NO Synthase (2) P2Y Receptor (1) Parasite (1) Phosphodiesterase (PDE) (1) Potassium Channel (1) Protease Activated Receptor (PAR) (2) RIP kinase (1)
By Research Areas:	Cancer (9) Cardiovascular Disease (3) Endocrinology (2) Infection (8) Inflammation/Immunology (15) Metabolic Disease (3) Neurological Disease (4)

By Targets:

Angiotensin Receptor (1)

Antibiotic (1)

Apoptosis (2)

Autophagy (1)

Bacterial (4)

Btk (1)

CD38 (1)

COX (7)

Cytochrome P450 (10)

Dopamine Receptor (1)

Drug Metabolite (3)

EGFR (1)

FAAH (1)

FABP (1)

Fungal (1)

GABA Receptor (1)

Glucocorticoid Receptor (2)

Histamine Receptor (1)

Histone Methyltransferase (2)

HIV (2)

IGF-1R (1)

IRAK (1)

JAK (1)

Keap1-Nrf2 (1)

Microtubule/Tubulin (1)

Mitophagy (1)

NO Synthase (2)

P2Y Receptor (1)

Parasite (1)

Phosphodiesterase (PDE) (1)

Potassium Channel (1)

Protease Activated Receptor (PAR) (2)

RIP kinase (1)

By Research Areas:

Cancer (9)

Cardiovascular Disease (3)

Endocrinology (2)

Infection (8)

Inflammation/Immunology (15)

Metabolic Disease (3)

Neurological Disease (4)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: LXR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N5132

(-)-Fenchone	Others	Others
(-)-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 .

HY-112690A

Pradefovir mesylate 1 Publications Verification Remofovir mesylate	Cytochrome P450	Metabolic Disease
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a K_m of 60 μM.

HY-N8094

Kushenol M	Cytochrome P450	Others
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 .

HY-150578

Keap1-Nrf2-IN-12	Keap1-Nrf2	Inflammation/Immunology
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-B0794S

AZ7550-d5	EGFR IGF-1R Drug Metabolite	Others
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].

HY-16718

Dagrocorat PF-00251802	Glucocorticoid Receptor Cytochrome P450	Inflammation/Immunology Endocrinology
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 (K_i=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .

HY-16718A

Dagrocorat hydrochloride PF-00251802 hydrochloride	Glucocorticoid Receptor Cytochrome P450	Inflammation/Immunology Endocrinology
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 (K_i=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .

HY-100644

Trimethoprim N-oxide Trimethoprim 1-N-oxide
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 .

HY-B0476

Phenacetin Acetophenetidin	COX	Inflammation/Immunology
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 .

HY-N1483

Guanfu base A	Potassium Channel	Cardiovascular Disease
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a K_i of 1.20 μM in human liver microsomes (HLMs) and a K_i of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (K_i of 0.38 μM) and dog (K_i of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .

HY-N11676

6-Hydroxy-TSU-68	Drug Metabolite	Cancer
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 .

HY-N11677

7-Hydroxy-TSU-68	Drug Metabolite	Others
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 .

HY-129105

Clomethiazole 2 Publications Verification	GABA Receptor Cytochrome P450	Neurological Disease
Chlormethiazole is an potent and orally active GABA_A 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 .

HY-146111

IRAK4-IN-13	IRAK	Cancer
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 .

HY-163032

FABP4-IN-3	FABP	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
FABP4-IN-3 (compound C3) is a highly selective FABP4 inhibitor (FABP4 K_i = 25 ± 3 ^a nM, FABP3 K_i = 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 .

HY-139721

Tenofovir-C3-O-C15-CF3 ammonium	HIV	Infection
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.

HY-151957

Antitubercular agent 34	Bacterial	Infection
Antitubercular agent 34 (compound 42g) is an antitubercular agent. Antitubercular agent 34 inhibits the growth of Mtb_H37Rv 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 .

HY-B0476S

Phenacetin-d5 Acetophenetidin-d₅	COX	Inflammation/Immunology
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].

HY-157931

Anticancer agent 192	Histamine Receptor	Neurological Disease
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 .

HY-10864

URB-597 4 Publications Verification KDS-4103	FAAH Autophagy Mitophagy	Neurological Disease
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 .

HY-17614

Ezutromid SMT C1100; BMN 195; VOX-C1100	Cytochrome P450	Others
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 .

HY-B0476S1

Phenacetin-13C	COX	Inflammation/Immunology
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].

HY-B0476R

Phenacetin (Standard) Acetophenetidin (Standard)	COX	Inflammation/Immunology
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 .

HY-149481

D4R agonist-1	Dopamine Receptor	Neurological Disease
D4R agonist-1 (Compound 16f) is a D4R partial agonist (K_i: 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 .

HY-143255

Enpp-1-IN-11	Phosphodiesterase (PDE)	Cancer
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an K_i 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 .

HY-143326

Antibacterial agent 83	Bacterial	Infection
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 .

HY-162408

PAR4 antagonist 3	Protease Activated Receptor (PAR)	Others
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 T_1/2 of 97.6 min .

HY-162409

PAR4 antagonist 4	Protease Activated Receptor (PAR)	Others
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 T_1/2 of 42.5 min .

HY-152118

CYP1B1-IN-4	Cytochrome P450	Cancer
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 .

HY-150508

MK-0159	CD38	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 .

HY-149920

Anticancer agent 98	Microtubule/Tubulin	Cancer
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (K_d=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 t_1/2>300 min .

HY-N0904

Ginsenoside C-K 3 Publications Verification Ginsenoside compound K; Ginsenoside K	COX NO Synthase Cytochrome P450	Inflammation/Immunology
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.

HY-151958

Antitubercular agent-35	Bacterial	Infection
Antitubercular agent-35 (compound 42l) is an antitubercular agent. Antitubercular agent-35 inhibits the growth of Mtb_H37Rv 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 .

HY-162238

OSM-S-106	Parasite	Infection
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 .

HY-147754

JAK3/BTK-IN-6	Btk JAK	Inflammation/Immunology
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 .

HY-123639

LM-4108 N-(2-Phenylethyl)-indomethacin amide	COX	Inflammation/Immunology Cancer
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 .

HY-N7454

Anhydroerythromycin A	Antibiotic Bacterial	Infection
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.

HY-146410

AT2R antagonist 1	Angiotensin Receptor	Others
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 K_i 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 .

HY-153394

Aflatoxin Q1	Fungal	Infection
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 .

HY-157325

RIPK2-IN-5	RIP kinase	Inflammation/Immunology
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 .

HY-N0904R

Ginsenoside C-K (Standard) Ginsenoside compound K(Standard); Ginsenoside K (Standard)	COX NO Synthase Cytochrome P450	Inflammation/Immunology
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.

HY-139722

Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium	HIV	Infection
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.

HY-146486

P2Y2R/GPR17 antagonist 1	P2Y Receptor	Inflammation/Immunology
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 .

HY-155051

Antiproliferative agent-25	Apoptosis Histone Methyltransferase	Cancer
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 T_1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .

HY-155141

hCYP3A4-IN-1	Cytochrome P450	Cancer
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) .

HY-155050

PRMT5-IN-31	Apoptosis Histone Methyltransferase	Cancer
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 (T_1/2: 132.4 min) .

Cat. No.	Product Name	Category	Target	Chemical Structure