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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
233 Results for "
peripherally active
" in MedChemExpress (MCE) Product Catalog:
Products (233)
233 Results for "peripherally active" in MCE Product Catalog:
97
97 Publications Verification
Synonyms: Isoproterenol hydrochloride
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Isoprenaline is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
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97 Publications Verification
Cat. No.: HY-108353A
CAS No.: 299-95-6
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Exendin‑4 (Exenatide) is an orally active, blood-brain barrier-permeable glucagon-like peptide-1 receptor (GLP‑1 receptor) agonist that resists degradation mediated by dipeptidyl peptidase IV. Exendin‑4 mediates multiple glucose-regulating effects, including stimulation of glucose-dependent insulin secretion, inhibition of glucagon production, increase in β-cell mass, delay of gastric emptying, reduction of food intake, improvement of peripheral insulin sensitivity, and restoration of normal islet structure. Exendin‑4 inhibits oxidative stress, alleviates inflammatory responses, and reduces neuronal apoptosis. Exendin‑4 reduces the aggregation level of mutant huntingtin, improves motor function, prolongs survival time, and regulates the expression levels of leptin and ghrelin. Exendin‑4 can be used in research related to type 2 diabetes, acute ischemic stroke, and Huntington's disease .
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72 Cited Publications
Synonyms: Exenatide acetate
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Exendin-4 acetate (Exenatide acetate) is an orally active, blood-brain barrier-permeable glucagon-like peptide-1 receptor (GLP‑1 receptor) agonist that resists degradation mediated by dipeptidyl peptidase IV. Exendin-4 acetate mediates multiple glucose-regulating effects, including stimulation of glucose-dependent insulin secretion, inhibition of glucagon production, increase in β-cell mass, delay of gastric emptying, reduction of food intake, improvement of peripheral insulin sensitivity, and restoration of normal islet structure. Exendin-4 acetate inhibits oxidative stress, alleviates inflammatory responses, and reduces neuronal apoptosis. Exendin-4 acetate reduces the aggregation level of mutant huntingtin, improves motor function, prolongs survival time, and regulates the expression levels of leptin and ghrelin. Exendin-4 acetate can be used in research related to type 2 diabetes, acute ischemic stroke, and Huntington's disease .
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33 Cited Publications
Synonyms: Clopidogrelum
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Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
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Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine .
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Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with Ki valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE2 (HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea .
11
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Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis .
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11 Cited Publications
Synonyms: BAF-312 hemifumarate
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Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis .
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Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
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8 Cited Publications
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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 .
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5
5 Cited Publications
Synonyms: P505-15; PRT-2607; BIIB-057
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PRT062607 (P505-15; PRT-2607) is an orally active ATP-competitive Syk inhibitor with an IC50 value of 1 nM, and exhibits at least 80-fold selectivity over other kinases. PRT062607 blocks B cell antigen receptor-mediated activation, Fcε receptor 1-mediated basophil degranulation and microglial phagocytosis, and induces caspase-dependent apoptosis and microglial death. PRT062607 inhibits tumor growth and peripheral nerve injury-induced mechanical allodynia, and prevents neuronal loss. PRT062607 can be used in research related to rheumatoid arthritis, chronic lymphocytic leukemia, non-Hodgkin's lymphoma, neurodegenerative diseases and neuropathic pain .
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4 Cited Publications
Synonyms: EMA401; PD-126055; (S)-EMA400
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Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
3
3 Cited Publications
Cat. No.: HY-18977
CAS No.: 1380424-42-9
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KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH .
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Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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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
