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rat and mouse liver microsomes

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By Targets:	Aldehyde Dehydrogenase (ALDH) (1) Angiotensin Receptor (1) CD38 (1) Chloride Channel (1) COX (1) Endogenous Metabolite (2) Parasite (1) Progesterone Receptor (1) TRP Channel (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (1)
Click Chemistry:	Alkynes (1)

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Click Chemistry

Targets Recommended: LXR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150508

MK-0159 1 Publications Verification	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-153508

ANO1-IN-4	Chloride Channel	Others
ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC₅₀ of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .

HY-128268

PFK-IN-1	Parasite	Infection
PFK-IN-1 (compound 1) is a phosphofructokinase (PFK) inhibitor, with IC₅₀ values of 0.41 and 0.23 μM against T.brucei and T.cruzi PFK, respectively, and an ED₅₀ of 15.18 μg/mL for T.brucei. The half-lives of PFK-IN-1 in rat and mouse liver microsomes are 9.7 and 408 minutes, respectively .

HY-151229

S-Methyl-N,N-diethylthiolcarbamate DETC-Me; DDTC-Me; Diethyldithiocarbamic acid methyl ester	Aldehyde Dehydrogenase (ALDH)	Metabolic Disease
S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) is the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram (HY-B0240). It is produced by the methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) inhibits rat liver low Km aldehyde dehydrogenase (ALDH) (ID50=15.5 mg/kg). When administered at a dose of 20.6 mg/kg, it decreases mean arterial pressure (MAP) and increases heart rate in rats during ethanol stimulation.

HY-B1341

Norethynodrel Enidrel; SC-4642; NSC 15432	Endogenous Metabolite Progesterone Receptor	Cancer
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .

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-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-173024

TRPC4/5-IN-3	TRP Channel	Neurological Disease
TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC₅₀ of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC₅₀ of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .

HY-182255

ED-594	Endogenous Metabolite	Others
ED-594 is the glucuronide form of NB-506. ED-594 is one of the major metabolites of NB-506 in rat bile, mouse liver microsomes, rat liver microsomes and human liver microsomes .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1341

Norethynodrel Enidrel; SC-4642; NSC 15432	Structural Classification Classification of Application Fields Endogenous metabolite Disease Research Fields Endocrinology Steroids Source Classification	Endogenous Metabolite Progesterone Receptor
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .

Cat. No.	Product Name		Classification

HY-B1341

Norethynodrel Enidrel; SC-4642; NSC 15432		Alkynes
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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rat and mouse liver microsomes

Inhibitors & Agonists

NaturalProducts

Click Chemistry

Natural
Products