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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
3017 Results for "
modulating
" in MedChemExpress (MCE) Product Catalog:
Products (3017)
3017 Results for "modulating" in MCE Product Catalog:
Cat. No.: HY-101036R
CAS No.: 87-67-2
Category:
Cat. No.: HY-105854A
CAS No.: 23744-24-3
Target:
Ras MEK ERK PI3K Akt MMP Keap1-Nrf2 Heme Oxygenase (HO) Reactive Oxygen Species (ROS) Apoptosis
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Pipoxolan is an orally active smooth muscle relaxant, anti-inflammatory agent and anticancer agent. Pipoxolan modulates PI3K/AKT signaling pathways, and reduces the levels of Ras/MEK/p-ERK, MMP-2 and MMP-9. Pipoxolan inhibits pro-inflammatory transcription factor pathways, activates Nrf2/HO-1, and suppresses the production of pro-inflammatory mediators. Pipoxolan induces ROS generation, endogenous mitochondrial Apoptosis, and G0/G1 cell cycle arrest. Pipoxolan reduces cerebral infarction size and inhibits intimal hyperplasia. Pipoxolan can be used in research related to cerebral ischemia, intimal hyperplasia, oral squamous cell carcinoma, leukemia and lung cancer .
Cat. No.: HY-106980
CAS No.: 308123-60-6
Synonyms: (-)-18-Methoxycoronaridine
Research Areas:
18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) is an orally active and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist. 18-Methoxycoronaridine is an inhibitor of serotonin transporter (SERT) and norepinephrine transporter (NET), with IC50 values of 51.6 μM and 121 μM for SERT and NET, respectively. 18-Methoxycoronaridine inhibits the function of SERT and NET, promotes 5-HT3A receptor desensitization, blocks α3β4 nAChR, and modulates receptor signaling pathways associated with reinforcement. 18-Methoxycoronaridine also exhibits potent antiparasitic activity. 18-Methoxycoronaridine can be used in research related to depression, obesity, alcoholism, smoking addiction, and cutaneous leishmaniasis .
Cat. No.: HY-106980A
CAS No.: 266686-77-5
Synonyms: (-)-18-Methoxycoronaridine hydrochloride
Research Areas:
18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) hydrochloride is an orally active and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist. 18-Methoxycoronaridine hydrochloride is an inhibitor of serotonin transporter (SERT) and norepinephrine transporter (NET), with IC50 values of 51.6 μM and 121 μM for SERT and NET, respectively. 18-Methoxycoronaridine hydrochloride inhibits the function of SERT and NET, promotes 5-HT3A receptor desensitization, blocks α3β4 nAChR, and modulates receptor signaling pathways associated with reinforcement. 18-Methoxycoronaridine hydrochloride also exhibits potent antiparasitic activity. 18-Methoxycoronaridine hydrochloride can be used in research related to depression, obesity, alcoholism, smoking addiction, and cutaneous leishmaniasis .
Cat. No.: HY-107111R
CAS No.: 932373-87-0
Target:
Research Areas:
GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
Cat. No.: HY-107574R
CAS No.: 17328-16-4
Research Areas:
TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein Kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers .
Cat. No.: HY-109112R
CAS No.: 1239729-06-6
Synonyms: RP5063 (Standard)
Research Areas:
Brilaroxazine (Standard) is the analytical standard of Brilaroxazine. This product is intended for research and analytical applications. Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .
Cat. No.: HY-109546
CAS No.: 95382-33-5
Target:
Na+/K+ ATPase Interleukin Related Proton Pump Cytochrome P450 Bacterial Apoptosis Autophagy TNF Receptor Atg8/LC3
Research Areas:
Omeprazole (H 16868) magnesium is an orally active H +,K +-ATPase inhibitor and a proton pump inhibitor. Omeprazole magnesium competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole magnesium inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole magnesium 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 magnesium alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole magnesium aslo has neuroprotective and antibacterial effects .
Cat. No.: HY-114583
CAS No.: 1041478-78-7
Target:
Research Areas:
AMG-8562 is a selective, orally active transient receptor potential vanilloid 1 (TRPV1) modulator that inhibits the activation of rat TRPV1 by Capsaicin (HY-10448), Anandamide (HY-10863) and N-arachidonyldopamine (HY-110018), with IC50 values of 1.75, 9.29 and 3.87 nM, respectively. AMG-8562 blocks capsaicin-induced activation, potentiates pH5-induced activation and has no effect on heat-induced activation of rat TRPV1, whereas it completely blocks capsaicin- and heat-induced activation and partially blocks pH5-induced activation of human TRPV1. AMG-8562 can be used in studies of TRPV1 activation patterns, hyperalgesia and pain-related research .
Cat. No.: HY-117106
CAS No.: 200266-76-8
Target:
Research Areas:
PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
Synonyms: PF-06372865; CVL-865
Target:
Research Areas:
Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .
Cat. No.: HY-123382
CAS No.: 1695551-19-9
Target:
Research Areas:
GSK-1482160 isomer is the isomer of GSK-1482160 (HY-19888). GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
Cat. No.: HY-12502B
CAS No.: 111011-53-1
Synonyms: NZ-105 hydrochloride; (±)-Efonidipine hydrochloride
Target:
Research Areas:
Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Cat. No.: HY-129138R
CAS No.: 2611-67-8
Category:
Cat. No.: HY-131997
CAS No.: 89112-85-6
Target:
Research Areas:
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .
Research Areas:
MitoPBN is a AMPK/SIRT3/PGC-1α axis modulator, reactive oxygen species scavenger and mitochondrial function enhancer. MitoPBN increases the phosphorylation level of AMPK, restores SIRT3 expression and reverses the down-regulation of PGC-1α, thereby promoting mitochondrial biogenesis. MitoPBN regulates glucose metabolism, reduces blood glucose by inhibiting hepatic gluconeogenesis and increasing hepatic glucose uptake, while scavenging mitochondrial superoxide anion/hydrogen peroxide, maintaining membrane potential and increasing ATP production. MitoPBN also reduces cell apoptosis, improves sperm motility, survival rate and membrane integrity, but may induce reductive stress in cryopreserved sperm at high concentrations. MitoPBN is widely applicable to research related to diabetes and type 2 diabetes .
Cat. No.: HY-15446R
CAS No.: 802906-73-6
Synonyms: RG7090 (Standard); RO4917523 (Standard)
Target:
Research Areas:
Basimglurant (RG7090; RO4917523) (Standard) is the analytical standard of Basimglurant. This product is intended for research and analytical applications. Basimglurant is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [ 3H]-ABP688 (HY-110141)) and 35.6 nM (against [ 3H]-MPEP (HY-14609A)). Basimglurant inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant can be used in research on depression, fragile X syndrome, anxiety disorders, etc.
Cat. No.: HY-159007
CAS No.: 58213-75-5
Synonyms: R,S-1,3-Butanediol acetoacetate diester
Target:
Pyroptosis NF-κB NOD-like Receptor (NLR) Caspase Apoptosis Autophagy Reactive Oxygen Species (ROS) Oxidative Phosphorylation Interleukin Related
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
BD-AcAc2 (R,S-1,3-Butanediol acetoacetate diester) is an orally active, CNS-penetrant antiepileptic agent. BD-AcAc2 inhibits NF-κB, NLRP3 inflammasome, caspase-1/3, pyroptosis, apoptosis, and enhances autophagy. BD-AcAc2 exhibits antioxidant activity by modulating ROS, MDA, SOD, and GSH levels, and alleviates oxidative stress. BD-AcAc2 mitigates chronic colitis, counteracts Dextran Sodium Sulfate (DSS)-induced pathology, protects against central nervous system oxygen toxicity and acute lung injury, and exhibits anti-seizure efficacy. BD-AcAc2 can be used for the research of colitis, sarcopenia, acute lung injury, seizure, and obesity .
Cat. No.: HY-160550
CAS No.: 3018836-86-4
Target:
Research Areas:
DPM-1003 is a modulator of protein tyrosine phosphatase 1B (PTP1B) and C-X-C chemokine receptor 4 (CXCR4). DPM-1003 binds to the non-catalytic disordered C-terminal fragment of PTP1B. DPM-1003 inhibits the PI3Kγ-mediated AKT/mTOR signaling pathway downstream of CXCR4. DPM-1003 improves the survival rate of mice in a transfusion-related acute lung injury model, and exerts a lung injury protective effect in preclinical mouse models of acute lung injury and sepsis. DPM-1003 can be used in research related to acute lung injury, acute respiratory distress syndrome, transfusion-related acute lung injury and sepsis .
Cat. No.: HY-16443
CAS No.: 173534-37-7
Target:
Research Areas:
S-4048 is a glucose-6-phosphate translocase modulator and hypoglycemic agent. S-4048 is taken up by hepatocytes via OATP-1 and is rapidly eliminated via the hepatobiliary system in rats. S-4048 blocks glucose-6-phosphate translocase, prevents glucose-6-phosphate from entering the endoplasmic reticulum, and thereby interferes with the glucose-6-phosphatase system (i.e., the final step of hepatic gluconeogenesis and glycogenolysis) to regulate hepatic glucose production. S-4048 completely inhibits glucose production from pyruvate in GLUT2-deficient hepatocytes without affecting the release of cytoplasmic glucose. S-4048 effectively reduces blood glucose levels in rats and has been used in studies related to type 2 diabetes .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
