157 Results for "

CYP2D6

" in MedChemExpress (MCE) Product Catalog:
Products (157)

157 Results for "CYP2D6" in MCE Product Catalog:

19
19 Publications Verification
Cat. No.: HY-122272
CAS No.: 61869-08-7
Purity:  99.92%
Synonyms: BRL29060
Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions .
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19
19 Publications Verification
Cat. No.: HY-B0492
CAS No.: 78246-49-8
Synonyms: BRL29060 hydrochloride; BRL29060A
Paroxetine (BRL29060) hydrochloride is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine hydrochloride inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine hydrochloride is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine hydrochloride is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions .
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11
11 Cited Publications
Cat. No.: HY-B0492A
CAS No.: 110429-35-1
Synonyms: BRL29060 hydrochloride hemihydrate; BRL29060A hemihydrate
Paroxetine (BRL29060) hydrochloride hemihydrate is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine hydrochloride hemihydrate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine hydrochloride hemihydrate is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine hydrochloride hemihydrate is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions .
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10
10 Cited Publications
Cat. No.: HY-B0113
CAS No.: 73590-58-6
Synonyms: H 16868
Omeprazole (H 16868) is an orally active H +,K +-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects .
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6
6 Cited Publications
Cat. No.: HY-50722
CAS No.: 357400-13-6
Synonyms: NNC 55-0396 dihydrochloride
NNC 55-0396 (NNC 55-0396 dihydrochloride) is a blood-brain-barrier-permeable T-type Ca 2+ channel inhibitor and pan-P450 inhibitor. NNC 55-0396 selectively inhibits T-type Ca 2+ channels, suppresses HIF-1α expression and stability and inhibits Kv currents. NNC 55-0396 reduces brain infarct and attenuates neurological dysfunction. NNC 55-0396 inhibits the activity of multiple P450 enzymes. NNC 55-0396 (free base) can be used for the research of brain injury, hypertension, and glioblastoma .
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3
3 Cited Publications
Cat. No.: HY-18719A
CAS No.: 1032008-74-4
Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
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3
3 Cited Publications
Cat. No.: HY-18719
CAS No.: 112093-28-4
Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
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2
2 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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2
2 Cited Publications
Cat. No.: HY-N2260
CAS No.: 5853-29-2
Synonyms: (-)-Cephaeline dihydrochloride; NSC 32944
Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
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2
2 Cited Publications
Cat. No.: HY-12753A
CAS No.: 197431-02-0
Purity:  98.73%
Synonyms: SR35021 hydrochloride
Debutyldronedarone hydrochloride (SR35021 hydrochloride) is a Cytochrome P450 enzyme inhibitor and a Thyroid Hormone Receptor inhibitor, and it is a metabolite of Dronedarone (HY-A0016). Debutyldronedarone hydrochloride inhibits the binding of T3 to TRα1 and TRβ1. Debutyldronedarone hydrochloride reduces the incidence of reperfusion-induced ventricular fibrillation in anesthetized rats, while decreasing their heart rate and blood pressure. Debutyldronedarone hydrochloride can be used in studies related to ventricular fibrillation and atrial fibrillation .
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1
1 Cited Publications
Cat. No.: HY-N0043
CAS No.: 52705-93-8
Synonyms: Gypenoside VIII
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
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1
1 Cited Publications
Cat. No.: HY-105124A
CAS No.: 60398-91-6
Purity:  98.03%
Synonyms: Ro 3-4787 hydrochloride
Target:  

Adrenergic Receptor

Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
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1
1 Cited Publications
Cat. No.: HY-105124
CAS No.: 54340-62-4
Purity:  99.17%
Synonyms: Ro 3-4787
Target:  

Adrenergic Receptor

Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
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1
1 Cited Publications
Cat. No.: HY-N2425
CAS No.: 86831-54-1
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
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1
1 Cited Publications
Cat. No.: HY-N0598
CAS No.: 53963-43-2
Synonyms: 20(S)-Ginsenoside F1
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
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1
1 Cited Publications
Cat. No.: HY-N2129
CAS No.: 4846-19-9
N-Nornuciferine is an orally active, blood-brain barrier-permeable CYP2D6 inhibitor, with an IC50 of 3.76 μM and a Ki of 2.34 μM against human CYP2D6. N-Nornuciferine also acts as a BChE inhibitor, showing an IC50 of 5.6 μM in mice . N-Nornuciferine can be used in the research of neurological-related diseases .
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1
1 Cited Publications
Cat. No.: HY-N2382
CAS No.: 81917-50-2
Polyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. Polyphyllin H potently inhibits the activities of CYP1A2 (IC50 = 6.44 μM, competitive), CYP2D6 (IC50 = 13.88 μM, competitive) and CYP3A4 (IC50 = 4.52 μM, non-competitive, time-dependent). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel .
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1
1 Cited Publications
Cat. No.: HY-N0241
CAS No.: 85571-15-9
Rhodionin is an orally active, multifunctional antivirulence and cytoprotective agent that targets and inhibits Lipase, sortase A (SrtA), CYP2D6 (IC50=0.761 μM), AChE (IC50=2.43-57.5 μM), and DPPH free radicals (IC50=19.49 μM). Rhodionin is isolable from the roots of Rhodiola crenulata. Rhodionin reduces postprandial serum triglyceride levels in mice by inhibiting lipase activity. Rhodionin also binds directly to SrtA to inhibit its transpeptidase activity, thereby reducing the fibrinogen adhesion and surface protein A levels of MRSA, effectively inhibiting biofilm formation and protecting against MRSA-induced cell damage. Rhodionin improves the survival rate of infected mice without affecting MRSA growth, and finds wide application in studies related to hyperlipidemia, exogenous obesity, and pneumonia induced by methicillin-resistant Staphylococcus aureus (MRSA) .
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1
1 Cited Publications
Cat. No.: HY-100665
CAS No.: 129722-25-4
Purity:  99.66%
Synonyms: OPC-14857; DM-14857
Research Areas:  

Neurological Disease

Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D2/D3 receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin 5-HT1A, 5-HT2A and 5-HT2B receptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole .
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1
1 Cited Publications
Cat. No.: HY-12242
CAS No.: 67469-81-2
Purity:  99.45%
Target:  

Dopamine Transporter

Research Areas:  

Neurological Disease

GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice .
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