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monkey liver microsomes

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By Targets:	11β-HSD (1) 5-HT Receptor (1) Acyltransferase (2) Bcl-2 Family (1) Bradykinin Receptor (1) CXCR (1) Cytochrome P450 (1) Factor XI (1) HIV (1) Kallikrein (1) P2X Receptor (1) Potassium Channel (1) Pregnane X Receptor (PXR) (1) Toll-like Receptor (TLR) (1) UGT (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (3) Infection (1) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (2)

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Targets Recommended: LXR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111358

TLR7 agonist 1	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 1 is a selective TLR7 agonist with an LEC value of 90 nM. TLR7 agonist 1 activates downstream immune regulation and shows no activity against TLR8. TLR7 agonist 1 induces endogenous IFN-α production in mice .

HY-112487

Sandoz 58-035	Acyltransferase	Metabolic Disease
Sandoz 58-035 is a selective acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. Sandoz 58-035 inhibits this enzyme in intact cells and isolated microsomal fractions. Sandoz 58-035 blocks the esterification of exogenous vesicle-derived cholesterol and the incorporation of oleic acid into cellular cholesterol esters, reducing the formation and accumulation of cholesterol esters. Sandoz 58-035 causes a slight increase in cellular free cholesterol, and at high concentrations, it also causes a slight reduction in overall cellular protein synthesis. Sandoz 58-035 can be used in studies related to cellular cholesterol regulation .

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-150519

FXIa/Plasma kallikrein-IN-1	Factor XI Kallikrein	Cardiovascular Disease
FXIa/Plasma kallikrein-IN-1 is an inhibitor of coagulation factor XIa (FXIa) and plasma kallikrein with K_i values of 187.70 nM and 151.6 nM, respectively. FXIa/Plasma kallikrein-IN-1 can be used in the research of thromboembolic diseases .

HY-117428

INU-101	11β-HSD	Metabolic Disease
INU-101 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .

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-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-162074

Nipamovir	HIV	Infection
Nipamovir is an anti-HIV prodrug. Nipamovir is cleaved in vivo by glutathione and other active thiols. Nipamovir inhibits the replication of HIV-1_RF and HIV-1_92HT599 in cells, with EC₅₀ values of 3.64 μM and 3.23 μM, respectively. Nipamovir can be used in studies related to HIV infection .

HY-182349

Bax activator-2	Bcl-2 Family	Cancer
Bax activator-2 (compound 27c) is a pro-apoptotic agent targeting BAX, with an IC₅₀ of 0.30 μmol/L against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, caspase-3/9 cleavage and PARP cleavage, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against various cancer cell lines, shows reduced cytotoxicity in BAX-knockout A549 cells, and has low cytotoxicity against non-cancerous cell lines. Bax activator-2 can be used in studies related to acute myeloid leukemia and solid tumors .

HY-124183

SX-576	CXCR	Inflammation/Immunology
SX-576 is a CXCR1 and CXCR2 antagonist with IC₅₀ values of 31 nM and 21 nM, respectively. SX-576 inhibits neutrophil infiltration in a rat model of pulmonary inflammation. SX-576 can be used in studies related to pulmonary inflammation .

HY-122163

MK-3901	P2X Receptor UGT Cytochrome P450 Pregnane X Receptor (PXR)	Neurological Disease
MK-3901 is a selective P2X3 receptor antagonist with an IC₅₀ of 24 nM. MK-3901 inhibits UGT1A1 (with an IC₅₀ of 1 μM) and CYP2C9 (with an IC₅₀ of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain .

HY-182440

AZD3783	5-HT Receptor	Neurological Disease
AZD3783 is an orally active, blood-brain barrier-penetrant 5-HT₁B receptor antagonist. AZD3783 reverses agonist-induced hypothermia, inhibits separation-induced vocalizations in guinea pig pups, and acts as a moderately permeable glycoprotein substrate with moderate clearance. AZD3783 inhibits hERG channel activity. AZD3783 is applicable for research on depression, anxiety disorders, and other psychiatric diseases associated with serotonergic neurotransmission .

Guanfu base A	Cardiovascular Disease Alkaloids Classification of Application Fields Other Alkaloids Ranunculaceae Aconitum carmichaeli Debx. Plants Disease Research Fields Source Classification	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 .

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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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monkey liver microsomes

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