262 Results for "

microsome

" in MedChemExpress (MCE) Product Catalog:
Products (262)

262 Results for "microsome" in MCE Product Catalog:

11
11 Publications Verification
Cat. No.: HY-103312
CAS No.: 88903-69-9
Purity:  ≥99.0%
Synonyms: (-)-Xestospongin C
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca 2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca 2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca 2+ signaling in neuronal and nonneuronal cells .
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6
6 Cited Publications
Cat. No.: HY-15295
CAS No.: 881681-01-2
Purity:  101.1%
Synonyms: TAK-438
Target:  

Proton Pump

Research Areas:  

Infection Inflammation/Immunology

Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease .
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6
6 Cited Publications
Cat. No.: HY-100007A
CAS No.: 1957202-44-6
Synonyms: TAK-438 hydrochloride
Target:  

Proton Pump Bacterial

Research Areas:  

Infection Endocrinology Cancer

Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan hydrochloride inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan hydrochloride is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride can be used for eradication of Helicobacter pylori .
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6
6 Cited Publications
Cat. No.: HY-100007
CAS No.: 881681-00-1
Purity:  99.40%
Synonyms: TAK-438 free base
Target:  

Proton Pump Bacterial

Research Areas:  

Infection

Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori .
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5
5 Cited Publications
Cat. No.: HY-100432
CAS No.: 877963-94-5
Purity:  ≥98.0%
Target:  

PDI

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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5
5 Cited Publications
Cat. No.: HY-10864
CAS No.: 546141-08-6
Purity:  99.15%
Synonyms: KDS-4103
Target:  

FAAH Autophagy Mitophagy

Research Areas:  

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 .
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5
5 Cited Publications
Cat. No.: HY-N0904
CAS No.: 39262-14-1
Synonyms: Ginsenoside compound K; Ginsenoside K
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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4
4 Cited Publications
Cat. No.: HY-129105
CAS No.: 533-45-9
Purity:  98.65%
Research Areas:  

Neurological Disease

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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4
4 Cited Publications
Cat. No.: HY-A0296
CAS No.: 6001-74-7
Synonyms: Clomethiazole hydrochloride
Target:  

Cytochrome P450

Research Areas:  

Neurological Disease

Clomethiazole hydrochloride is a potent and orally active GABAA agonist . Clomethiazole hydrochloride inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Clomethiazole hydrochloride is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
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3
3 Cited Publications
Cat. No.: HY-101016
CAS No.: 34450-18-5
Purity:  ≥98.0%
Research Areas:  

Cardiovascular Disease

17-ODYA is a CYP450 ω-hydroxylase inhibitor. 17-ODYA is also a potent inhibitor (IC50<100 nM) of the formation of 20-hydroxyeicosatetraenoic acid (20-HETE), epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids by rat renal cortical microsomes incubated with arachidonic acid. 17-ODYA completely attenuates the isoproterenol (ISO)-induced apoptosis, and necrosis in cultured cardiomyocytes . 17-ODYA 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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3
3 Cited Publications
Cat. No.: HY-D0837
CAS No.: 288-32-4
Synonyms: Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene
Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
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3
3 Cited Publications
Cat. No.: HY-15163
CAS No.: 1204918-72-8
Synonyms: TG02; SB1317
Target:  

JAK CDK FLT3

Research Areas:  

Cancer

Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
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1
1 Cited Publications
Cat. No.: HY-B0476
CAS No.: 62-44-2
Synonyms: Acetophenetidin
Target:  

COX

Research Areas:  

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 .
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1
1 Cited Publications
Cat. No.: HY-N4070
CAS No.: 73566-30-0
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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1
1 Cited Publications
Cat. No.: HY-N4071
CAS No.: 71385-83-6
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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1
1 Cited Publications
Cat. No.: HY-112690A
CAS No.: 625095-61-6
Purity:  99.53%
Synonyms: Remofovir mesylate
Target:  

Cytochrome P450

Research Areas:  

Infection 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 Km of 60 μM.
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1
1 Cited Publications
Cat. No.: HY-107460
CAS No.: 1198408-78-4
Purity:  ≥99.0%
Target:  

Ephrin Receptor

Research Areas:  

Cancer

LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
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1
1 Cited Publications
Cat. No.: HY-126687
CAS No.: 2259318-52-8
Purity:  95.97%
Research Areas:  

Cancer

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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1
1 Cited Publications
Cat. No.: HY-150508
CAS No.: 2641484-61-7
Purity:  98.60%
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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1
1 Cited Publications
Cat. No.: HY-N3807
CAS No.: 19914-20-6
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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