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liver microsome

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Acyltransferase (5) ADC Cytotoxin (2) Adenosine Receptor (2) Adrenergic Receptor (1) Androgen Receptor (1) Angiotensin Receptor (1) Antibiotic (2) Apoptosis (3) Autophagy (1) Bacterial (9) Bcl-2 Family (2) BCRP (1) Bradykinin Receptor (1) Btk (1) CD38 (1) COX (6) Cytochrome P450 (14) Dopamine Receptor (1) Drug Metabolite (6) Drug-Linker Conjugates for ADC (3) EGFR (1) Endogenous Metabolite (3) Ephrin Receptor (1) ERK (3) FAAH (1) FABP (1) FGFR (1) Fungal (1) GABA Receptor (2) Glucocorticoid Receptor (2) GnRH Receptor (1) Histamine Receptor (3) Histone Methyltransferase (2) HIV (5) HIV Protease (1) IGF-1R (1) IRAK (1) Isotope-Labeled Compounds (1) JAK (2) Keap1-Nrf2 (1) LRRK2 (1) MCHR1 (GPR24) (1) MEK (1) Microtubule/Tubulin (1) Mitophagy (1) Monoamine Oxidase (2) NF-κB (1) NO Synthase (1) NOD-like Receptor (NLR) (1) Opioid Receptor (1) P2Y Receptor (1) Parasite (2) PARP (2) PDI (1) Phosphodiesterase (PDE) (3) Phospholipase (1) Potassium Channel (2) PPAR (1) Protease Activated Receptor (PAR) (2) Proton Pump (1) PTHR (1) Ras (1) Reverse Transcriptase (1) RIP kinase (1) Sigma Receptor (1) Survivin (2) Tau Protein (1) Tryptophan Hydroxylase (1)
By Research Areas:	Cancer (32) Cardiovascular Disease (9) Endocrinology (6) Infection (22) Inflammation/Immunology (23) Metabolic Disease (17) Neurological Disease (15)
Click Chemistry:	DBCO (1)

120

Inhibitors & Agonists

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: LXR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-10864

URB-597 5 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-169258

PDE4-IN-21	Phosphodiesterase (PDE)	Metabolic Disease
PDE4-IN-21 (Compound L19) is a poetent PDE4 inhibitor, with an IC₅₀ of 0.48 μM. PDE4-IN-21 exhibits good inhibitory activity and remarkable metabolic stability in rat liver microsomes .

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-149395

MmpL3-IN-3	Bacterial	Infection
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 .

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-100644

Trimethoprim N-oxide Trimethoprim 1-N-oxide	Drug Metabolite	Infection
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-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-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-N5132R

(-)-Fenchone (Standard)	Others	Others
(-)-Fenchone (Standard) is the analytical standard of (-)-Fenchone. This product is intended for research and analytical applications. (-)-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-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-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-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) .

HY-123370

FR-167356	Proton Pump	Metabolic Disease Cancer
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 .

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-W741611

Dehydro Warfarin NSC 289346	Others	Metabolic Disease
Dehydro warfarin is a metabolite of (±)-warfarin. It is formed from (±)-warfarin by rat liver microsomes.

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-112690

Pradefovir	Cytochrome P450	Metabolic Disease
Pradefovir 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-W003371

CGP 44 645	Drug Metabolite	Others
CGP 44 645 is the methanol metabolite of Letrozole (HY-14248) and is a molecular indicator for evaluating its metabolic kinetics in microsomes in vitro. Levels of CGP 44 645 in rat liver microsomes may be sex-specific .

HY-101627

YM17E	Acyltransferase	Metabolic Disease
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC₅₀ of 44 nM in rabbit liver microsomes in vitro.

HY-124098

Lignocaine N-oxide Lidocaine N-oxide	Others	Others
Lignocaine N-oxide (Lidocaine N-oxide) is a compound derived from the metabolism of lidocaine. Lidocaine can be metabolized to its N-oxide in rat liver microsomes.

HY-N6702

Enniatin A	Acyltransferase	Infection Cardiovascular Disease
Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 22 μM in an enzyme assay using rat liver microsomes .

HY-163291

AM4085	Bacterial	Infection
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 .

HY-B1311

Proadifen hydrochloride 1 Publications Verification SKF-525A; U-5446; RP-5171	Cytochrome P450 Monoamine Oxidase Bcl-2 Family Survivin PARP	Neurological Disease Inflammation/Immunology Cancer
Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC₅₀ value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .

HY-W003371R

CGP 44 645 (Standard)	Drug Metabolite	Others
CGP 44 645 (Standard) is the analytical standard of CGP 44 645. This product is intended for research and analytical applications. CGP 44 645 is the methanol metabolite of Letrozole (HY-14248) and is a molecular indicator for evaluating its metabolic kinetics in microsomes in vitro. Levels of CGP 44 645 in rat liver microsomes may be sex-specific .

HY-137580

N-Desmethyl Eletriptan	Others	Metabolic Disease
N-desmethyl Eletriptan is a metabolite of Eletriptan (HY-A0039). It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 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-126665

DMEA-PNU-159682	ADC Cytotoxin	Cancer
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 .

HY-B1311R

Proadifen hydrochloride (Standard)	Cytochrome P450 Monoamine Oxidase Bcl-2 Family Survivin PARP	Neurological Disease Inflammation/Immunology Cancer
Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases [4] .

HY-N4070

6"-O-Acetylgenistin	Others	Others
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 .

HY-N4071

6"-O-Acetyldaidzin	Others	Others
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 .

HY-126665A

DMEA-PNU-159682 dichloroacetate	ADC Cytotoxin	Cancer
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 .

HY-U00369

FCE 28654	Acyltransferase	Cardiovascular Disease
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.

HY-100432

LOC14 2 Publications Verification	PDI	Neurological Disease Inflammation/Immunology
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC₅₀ and K_d 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 .

HY-113777

22-HDHA 22-Hydroxy Docosahexaenoic acid; 22-OH DHA	Others	Metabolic Disease
22-HDHA is an oxidation product of docosahexaenoic acid.1 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.

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-40156

5-Fluoroindole	Bacterial	Infection
5-Fluoroindole is an antibacterial agent, that inhibits Mycobacterium tuberculosis with a MIC of 4.7 μM. 5-Fluoroindole exhibits metabolic stability in rat liver microsomes. 5-Fluoroindole exhibits anti-tuberculosis efficacy in mice .

HY-125568

Pyridoxatin	Others	Others
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 .

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-130238

(±)8-HDHA (±)8-HDoHE; 8-hydroxy Docosahexaenoic acid; (±)8-HDoHE	Endogenous Metabolite	Metabolic Disease
(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)8-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.

HY-130287

(±)16-HDHA (±)16-HDoHE; 16-hydroxy Docosahexaenoic acid; (±)16-HDoHE	Endogenous Metabolite	Metabolic Disease
(±)16-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)16-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.

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-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-153822

JG-23	Tau Protein	Neurological Disease
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 .

HY-15042

MK 0686	Bradykinin Receptor	Metabolic Disease
MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .

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-W040790S

2,6-Dimethylpyrazine-d6	Isotope-Labeled Compounds	Others
2,6-Dimethylpyrazine-d₆ is deuterated labeled Beauvericin (HY-N6739). Beauvericin is a Fusarium mycotoxin. Beauvericin inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 3 μM in an enzyme assay using rat liver microsomes .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N5132

(-)-Fenchone	Structural Classification Other Monoterpenes Classification of Application Fields Terpenoids Source classification Other Diseases Umbelliferae Plants Vernonia Schreb. Disease Research Fields	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-N4070

6"-O-Acetylgenistin	Structural Classification Flavonoids Classification of Application Fields Leguminosae Glycine max (L.) merr Source classification Other Diseases Phenols Polyphenols Plants Disease Research Fields Isoflavones	Others
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 .

HY-N4071

6"-O-Acetyldaidzin	Structural Classification Monophenols Flavonoids Classification of Application Fields Leguminosae Glycine max (L.) merr Source classification Other Diseases Phenols Plants Disease Research Fields Isoflavones	Others
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 .

HY-N1483

Guanfu base A	Cardiovascular Disease Alkaloids Classification of Application Fields Source classification Ranunculaceae Aconitum carmichaeli Debx. Plants Disease Research Fields	Potassium Channel
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-N8094

Kushenol M	Flavanonols Flavonoids Classification of Application Fields Leguminosae Source classification Other Diseases Phenols Polyphenols Plants Sophora flavescens Aiton Disease Research Fields	Cytochrome P450
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-N5132R

(-)-Fenchone (Standard)	Structural Classification Other Monoterpenes Terpenoids Source classification Umbelliferae Plants Vernonia Schreb.	Others
(-)-Fenchone (Standard) is the analytical standard of (-)-Fenchone. This product is intended for research and analytical applications. (-)-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-N6702

Enniatin A	Cardiovascular Disease Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields	Acyltransferase
Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 22 μM in an enzyme assay using rat liver microsomes .

HY-125568

Pyridoxatin	Alkaloids Structural Classification Microorganisms Classification of Application Fields Source classification Other Diseases Pyridine Alkaloids Disease Research Fields	Others
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 .

HY-N11676

6-Hydroxy-TSU-68	Structural Classification Alkaloids Monophenols Pyrrole Alkaloids Source classification Phenols Endogenous metabolite	Drug Metabolite
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	Structural Classification Alkaloids Monophenols Pyrrole Alkaloids Source classification Phenols Endogenous metabolite	Drug Metabolite
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-N3806

Enniatin B	Infection Cardiovascular Disease Alkaloids Microorganisms Classification of Application Fields Source classification Disease Research Fields	Acyltransferase ERK
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) .

HY-N6704

Enniatin A1	Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Anticancer Disease Research Fields Cancer	ERK Apoptosis
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 .

HY-N0904

Ginsenoside C-K 5 Publications Verification Ginsenoside compound K; Ginsenoside K	Panax ginseng C. A. Meyer Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Inflammation/Immunology Disease Research Fields Araliaceae	COX NO Synthase Cytochrome P450
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-N7454

Anhydroerythromycin A	Infection Structural Classification Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Endogenous metabolite Disease Research Fields	Antibiotic Bacterial
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-N3807

Enniatin B1 1 Publications Verification	Infection Cardiovascular Disease Alkaloids Structural Classification Microorganisms Classification of Application Fields Other Alkaloids Source classification Disease Research Fields	Acyltransferase ERK NF-κB
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 .

HY-N7454R

Anhydroerythromycin A (Standard)	Structural Classification Macrolide Antibiotics Antibiotics Source classification Antibacterial Disease Research Endogenous metabolite	Antibiotic Bacterial
Anhydroerythromycin A (Standard) is the analytical standard of Anhydroerythromycin A. This product is intended for research and analytical applications. 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.

Cat. No.	Product Name	Chemical Structure

HY-B0476S

Phenacetin-d5
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-B0794S

AZ7550-d5
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-W040790S

2,6-Dimethylpyrazine-d6
2,6-Dimethylpyrazine-d₆ is deuterated labeled Beauvericin (HY-N6739). Beauvericin is a Fusarium mycotoxin. Beauvericin inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 3 μM in an enzyme assay using rat liver microsomes .

HY-B0476S1

Phenacetin-13C
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-B0822S1

Fipronil-13C6

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.

Cat. No.	Product Name		Classification

HY-126691

DBCO-PEG4-VC-PAB-DMEA-PNU-159682		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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