65 Results for "

excessive activity

" in MedChemExpress (MCE) Product Catalog:
Products (65)

65 Results for "excessive activity" in MCE Product Catalog:

3
3 Cited Publications
Cat. No.: HY-W013375
CAS No.: 76721-89-6
Target:  

Neprilysin

Research Areas:  

Neurological Disease

Thiorphan is a selective neprilysin (NEP) inhibitor with an IC50 of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases .
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3
3 Cited Publications
Cat. No.: HY-18101A
CAS No.: 206996-13-6
Research Areas:  

Neurological Disease

BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .
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2
2 Cited Publications
Cat. No.: HY-N0541
CAS No.: 69884-00-0
Synonyms: Ginsenoside A1
Pseudoginsenoside F11 is an orally active neuroprotective agent. Pseudoginsenoside F11 reduces the expression of β-amyloid precursor protein, inhibits the production of 1-40, downregulates the expression of JNK2, p53 and activated Caspase 3, and restores the activities of SOD and Glutathione peroxidase. Pseudoginsenoside F11 inhibits the excessive activation of μ-Calpain and restores the level of neuronal Nitric oxide synthase. Pseudoginsenoside F11 reduces infarct volume, alleviates cerebral edema, decreases neuronal loss, improves neurological deficits and enhances long-term functional outcomes in transient cerebral ischemia models. Pseudoginsenoside F11 antagonizes Methamphetamine-induced behavioral deficits, dopamine level reduction and neurotoxicity without altering the baseline behaviors of normal mice. Pseudoginsenoside F11 can be used in studies related to Alzheimer's disease, transient cerebral ischemic injury and Methamphetamine-induced neurotoxicity .
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2
2 Cited Publications
Cat. No.: HY-N1970
CAS No.: 31721-94-5
5,7-Dihydroxychromone is a flavonoid compound with antioxidant properties. 5,7-Dihydroxychromone induces Nrf2 nuclear translocation, increases Nrf2/ARE binding activity, and up-regulates Nrf2-dependent antioxidant genes HO-1, NQO1, GCLc. 5,7-Dihydroxychromone attenuates excessive ROS generation, inhibits activated caspase-3, caspase-9, cleaved PARP expression, and prevents neuronal apoptosis and cell death. 5,7-Dihydroxychromone increases LXRα and PPARγ mRNA expression, induces preadipocyte differentiation, and regulates blood glucose levels. 5,7-Dihydroxychromone inhibits radial growth of soil pathogenic fungi, radicle elongation of select seedlings, and transiently inhibits Bradyrhizobium sp. growth in high mannitol medium. 5,7-Dihydroxychromone can be used for the research of Parkinson’s disease, type 2 diabetes mellitus and pathogenic fungal infection .
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1
1 Cited Publications
Cat. No.: HY-120868
CAS No.: 1454299-21-8
Purity:  99.17%
Target:  

MetAP

Research Areas:  

Metabolic Disease Cancer

TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC50 of 6 nM against MetAP2. TP-004 is a chemical probe. TP-004 suppresses MetAP2 enzymatic activity, blocks N-terminal methionine cleavage, impairs protein maturation and stability, and thereby inhibits cell proliferation and angiogenesis. TP-004 can be used for the study of tumors and diseases associated with excessive angiogenesis .
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Cat. No.: HY-14401
CAS No.: 787583-71-5
Purity:  99.88%
Synonyms: CLTX-305; JTT-305; MK-5442
Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1 .
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Cat. No.: HY-W007087
CAS No.: 6106-41-8
Target:  

GABA Receptor

Research Areas:  

Metabolic Disease

Valerate sodium is the sodium salt of valeric acid, a short-chain fatty acid, and exhibits oral activity. Valerate sodium reduces binge ethanol intake and decreases blood ethanol concentration in mice, while also exerting anxiolytic effects. Valerate sodium increases GABA levels, regulates epigenetics and alters gut microbiome function. Valerate sodium can be used in research related to excessive alcohol consumption .
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Cat. No.: HY-129724A
CAS No.: 2828433-34-5
Synonyms: ACTH-(11-13) acetate; Lys-Pro-Val acetate; H-Lys-Pro-Val-OH acetate
α-MSH (11-13) (ACTH-(11-13)) acetate is a C-terminal tripeptide of α-MSH that can cross the blood-brain barrier. α-MSH (11-13) acetate exhibits antipyretic, anti-inflammatory, and antibacterial activities. α-MSH (11-13) acetate also exerts neuroprotective effects after traumatic brain injury by inhibiting excessive activation of microglia and reducing neuronal apoptosis. α-MSH (11-13) acetate can be used in research related to traumatic brain injury, fever, and bacterial infections .
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Cat. No.: HY-W704574
CAS No.: 77102-28-4
Mergetpa is a reversible Arg-carboxypeptidase inhibitor with high affinity. Mergetpa reduces B1R. Mergetpa blocks the overexpression of IL-1β protein and mRNA in glucose-fed rats. Mergetpa significantly increases the expression of IL-1β protein in the renal cortex. Mergetpa is used to block the conversion of kinins and B2 receptor antagonists into metabolites lacking the C-terminal arginine. Mergetpa inhibits the time-dependent enhancement of the response of isolated rabbit aorta to bradykinin. Mergetpa preserves the chemotactic activity of full-length SDF-1α on cells. Mergetpa reverses hyperglycemia, excessive weight gain, elevated levels of oxidative stress markers and overexpression of inflammatory markers in glucose-fed rats .
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Cat. No.: HY-B0380
CAS No.: 39133-31-8
Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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Cat. No.: HY-B0380A
CAS No.: 34140-59-5
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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Cat. No.: HY-WAA0142
CAS No.: 2578-57-6
L-Prolylglycine is a proline-glycine dipeptide. L-Prolylglycine is absorbable through the jejunal and ileal mucosa. In streptozotocin (HY-13753)-induced diabetic mice, L-Prolylglycine reduces hepatic ALT activity and increases hepatic ALP activity. L-Prolylglycine prevents excessive elevation of blood glucose in diabetic mice. L-Prolylglycine is applicable to diabetes-related research .
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Cat. No.: HY-111083
CAS No.: 931695-79-3
Purity:  99.65%
Synonyms: CID23612552
Target:  

GPR55 PERK PKC ERK p38 MAPK

Research Areas:  

Metabolic Disease Cancer

ML191 (CID23612552) is a GPR55 antagonist. ML191 inhibits ERK phosphorylation and PKC β II translocation downstream of GPR55 signaling. ML191 suppresses LPI-induced activation of ERK1/2 and p38 MAPK signaling, blocks the transcription of RANKL-induced osteoclastogenesis markers, and reduces the bone resorption activity of mature osteoclasts promoted by RANKL. ML191 can be used to investigate diseases associated with bone degradation caused by excessive osteoclast activation, such as osteoporosis and bone damage during the formation stage of bone metastases .
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Cat. No.: HY-111178
CAS No.: 90280-13-0
Purity:  99.18%
Synonyms: BisfluoroModafinil; CRL-40940; NLS-4
Target:  

Dopamine Transporter

Research Areas:  

Neurological Disease

Lauflumide (BisfluoroModafinil) is a selective dopamine reuptake inhibitor and wake-promoting agent. Lauflumide inhibits the dopamine transporter (DAT). Lauflumide induces sustained wakefulness without eliciting hyperlocomotion, stereotypy or abnormal behaviors in Mus musculus (house mice). Lauflumide reduces non-rapid eye movement (NREM) sleep rebound in rats, modulates electroencephalogram (EEG) spectral composition, and produces anti-aggressive effects. Lauflumide alleviates circadian rhythm disturbances in rats, increases spontaneous activity in fatigued rats, and facilitates their recovery from severe fatigue. Lauflumide can be used in research related to excessive daytime sleepiness as well as chronic severe fatigue/chronic fatigue syndrome (CFS) .
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Cat. No.: HY-N1510
CAS No.: 22149-35-5
Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma . It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer .
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Cat. No.: HY-124452
CAS No.: 26605-16-3
Purity:  95.00%
Synonyms: Desferrioxamine E; Nocardamin
Nocardamine (Desferrioxamine E; Nocardamin) is a cyclic trihydroxamate siderophore with iron ion chelation, antioxidant, antibacterial and other activities. Nocardamine is synthesized by Pseudomonas stutzeri under iron-deficient conditions, and excessive iron ions significantly inhibit its biosynthesis process. Nocardamine increases the level of phosphorylated ERK protein, promotes nuclear translocation of β-catenin, and restores the downregulated expression of SIRT1 protein. Nocardamine alleviates cellular oxidative stress, reduces ROS content, and simultaneously repairs the ability to form mineralized nodules and the expression of osteogenic markers. Nocardamine induces FoxA gene transcription and protein expression to assist Pseudomonas aeruginosa in iron ion uptake; it also selectively inhibits the proliferation of mycobacteria. Nocardamine induces spindle-shaped morphological changes in BM-N4 insect cells, and sufficient iron ions inhibit this cellular morphological change. Nocardamine is suitable for research related to bacterial infections .
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Cat. No.: HY-121811
CAS No.: 484-33-3
Purity:  99.81%
Synonyms: Lanceolatin C
Pongamol (Lanceolatin C) is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol exhibits antibacterial activity. Pongamol alleviates oxidative stress, neuroinflammation, deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
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Cat. No.: HY-129724
CAS No.: 67727-97-3
Synonyms: ACTH-(11-13); Lys-Pro-Val; H-Lys-Pro-Val-OH
α-MSH (11-13) (ACTH-(11-13)) is a C-terminal tripeptide of α-MSH that can cross the blood-brain barrier. α-MSH (11-13) exhibits antipyretic, anti-inflammatory, and antibacterial activities. α-MSH (11-13) also exerts neuroprotective effects after traumatic brain injury by inhibiting excessive activation of microglia and reducing neuronal apoptosis. α-MSH (11-13) can be used in research related to traumatic brain injury, fever, and bacterial infections .
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Cat. No.: HY-W047191
CAS No.: 1198-69-2
D-Glucono-1,4-lactone is a derivative of D-gluconic acid (HY-Y0569C). D-Glucono-1,4-lactone can be isolated from fruits, vegetables, honey, kombucha and wine. D-Glucono-1,4-lactone inhibits thrombin-induced arachidonic acid peroxidation and platelet activation. D-Glucono-1,4-lactone reduces superoxide anion production in thrombin-activated platelets. D-Glucono-1,4-lactone exerts antioxidant activity on platelets under oxidative stress conditions and prevents excessive platelet activation through antioxidant mechanisms. D-Glucono-1,4-lactone can be used in research related to cardiovascular diseases .
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Cat. No.: HY-W145481A
CAS No.: 11078-30-1
Synonyms: Carob galactomannan
D-Galacto-D-mannan (Carob galactomannan) is an orally active Dectin-2 agonist. D-Galacto-D-mannan exerts antioxidant activity against hydroxyl radical generation. D-Galacto-D-mannan activates Dectin-2 to trigger downstream signaling pathways, promote the expression of immunoregulatory molecules, coordinate innate and adaptive immune responses, and inhibit excessive inflammatory responses by upregulating the expression of Sirtuin 1. When used as a vaccine adjuvant, D-Galacto-D-mannan induces cellular and humoral immune responses, promotes IFNγ secretion, increases antibody levels and virus neutralization titers, and elevates the levels of immunoglobulin G and A. D-Galacto-D-mannan can serve as an adjuvant for foot-and-mouth disease vaccines, enhance the vaccine-mediated ability of hosts to defend against viral infection in mice, and reduce local side effects at the inoculation site in pigs. D-Galacto-D-mannan can be used in the research of inflammatory and immune diseases, such as foot-and-mouth disease .
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