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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
238 Results for "
selective peripheral
" in MedChemExpress (MCE) Product Catalog:
Products (238)
238 Results for "selective peripheral" in MCE Product Catalog:
Cat. No.: HY-N18471B
CAS No.: 39929-27-6
Synonyms: 5,7-DHP creatinine sulfate
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5,7-Dihydroxytryptamine creatinine sulfate (5,7-DHT) is an autofluorescent (Ex ≈ 365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine creatinine sulfate can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine creatinine sulfate can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
Cat. No.: HY-P990197
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Cat. No.: HY-137055
CAS No.: 1171824-96-6
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
Cat. No.: HY-13224A
CAS No.: 758722-12-2
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AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
Cat. No.: HY-184108
CAS No.: 2486316-20-3
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ZL006-05 is an orally active, brain-penetrant nNOS–PSD-95 and α2-containing GABAA dual-target inhibitor. ZL006-05 blocks the nNOS-PSD-95 protein-protein interaction and selectively potentiatesα2-containing GABAA receptors. ZL006-05 attenuates central sensitization and strengthens inhibitory GABAergic synaptic transmission. ZL006-05 can be used for the study of neuropathic pain, cancer pain, chemotherapy-induced peripheral neuropathic pain, ischemic stroke, poststroke depression and anxiety .
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Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
Cat. No.: HY-100027
CAS No.: 127500-84-9
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Ro 41-1049 is a highly selective, reversible MAO-A inhibitor. Ro 41-1049 effectively blocks the Quinpirole (HY-B1752)-induced increase in dopamine D2-like receptor density in the nucleus accumbens and alters the pattern of behavioral sensitization, shifting animals' responses from enhanced motor activity to immobile self-directed gaping behavior. Tritium-labeled Ro 41-1049 serves as a high-affinity radioligand, enabling accurate mapping of the distribution and abundance of MAO-A in the central nervous system, peripheral organs, and human brain via quantitative enzyme autoradiography. Ro 41-1049 can be used for basic research on depression and other related diseases .
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Ro 41-1049 hydrochloride is a highly selective, reversible MAO-A inhibitor. Ro 41-1049 hydrochloride effectively blocks the Quinpirole (HY-B1752)-induced increase in dopamine D2-like receptor density in the nucleus accumbens and alters the pattern of behavioral sensitization, shifting animals' responses from enhanced motor activity to immobile self-directed gaping behavior. Tritium-labeled Ro 41-1049 hydrochloride serves as a high-affinity radioligand, enabling accurate mapping of the distribution and abundance of MAO-A in the central nervous system, peripheral organs, and human brain via quantitative enzyme autoradiography. Ro 41-1049 hydrochloride can be used for basic research on depression and other related diseases .
Cat. No.: HY-110206R
CAS No.: 1245626-05-4
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AM6545 (Standard) is the analytical standard of AM6545 (HY-110206). This product is intended for research and analytical applications. AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
Cat. No.: HY-14280R
CAS No.: 130929-57-6
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Entacapone (Standard) is the analytical standard of Entacapone. This product is intended for research and analytical applications. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
Cat. No.: HY-126031
CAS No.: 2055172-60-4
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(R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation .
Cat. No.: HY-177338
CAS No.: 2361424-97-5
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STING agonist-45 is a selective STING agonist (EC50 = 0.28 μM). STING agonist-45 activates the innate immune response through the cGAS-STING pathway, upregulating key markers such as p-TBK1 and IRF3. STING agonist-45 exhibits robust STING activation in human peripheral blood mononuclear cells (PBMCs), inducing the production of type I interferons (such as IFN-β) and downstream cytokines (such as TNF-α and IL-6). STING agonist-45 enhances anti-tumor immunity, inhibits tumor growth, and increases CD8 + T cell infiltration in mouse models. STING agonist-45 is promising for the study of STING-related diseases .
Cat. No.: HY-186072
CAS No.: 2771019-10-2
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
Cat. No.: HY-A0144AR
CAS No.: 943-17-9
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Etilefrine (Standard) is the analytical standard of Etilefrine. This product is intended for research and analytical applications. Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
Cat. No.: HY-B0197AR
CAS No.: 143388-64-1
Synonyms: GR-85548A hydrochloride (Standard)
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Cardiovascular Disease Neurological Disease Inflammation/Immunology
Naratriptan (GR-85548A) hydrochloride (Standard) is the analytical standard of Naratriptan hydrochloride (HY-B0197A). This product is intended for research and analytical applications. Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .
Cat. No.: HY-B0197AS
CAS No.: 1190021-64-7
Synonyms: GR-85548A d3
Cat. No.: HY-B0197S
CAS No.: 1190043-69-6
Synonyms: GR-85548A-d3-1
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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
