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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
236 Results for "
peripherally active
" in MedChemExpress (MCE) Product Catalog:
Products (236)
236 Results for "peripherally active" in MCE Product Catalog:
Cat. No.: HY-183244
CAS No.: 121412-39-3
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CGS 21595 is an orally active 5-lipoxygenase inhibitor that blocks the synthesis of 5-hydroxyeicosatetraenoic acid and leukotriene B4. CGS 21595 acts as a prodrug and metabolizes into CGS 19213. CGS 21595 induces lesions in the spinal nerve roots and sciatic nerves of rats, causing mild functional impairments including reduced grip strength, increased spread of the landing feet, and decreased motor activity. CGS 21595 exhibits dose-dependent neurotoxicity in rats, and induces reversible cytoplasmic hyaline droplets in the proximal renal tubules of both male and female rats. CGS 21595 can be used in studies of peripheral toxic neuropathy .
Cat. No.: HY-182333
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AChE-IN-112 is an acetylcholinesterase (AChE) inhibitor with an IC50 of 0.41 μM. AChE-IN-112 scavenges various reactive oxygen and reactive nitrogen species, including DPPH, ABTS, NO, hydroxyl and hydrogen peroxide free radicals. AChE-IN-112 can be used for the research of Alzheimer's disease .
Cat. No.: HY-184791
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AChE-IN-120 is a blood-brain barrier-permeable AChE inhibitor, with an IC50 of 0.91 μM and a Ki of 1.027 μM against human AChE. AChE-IN-120 exerts neuroprotective effects against oxidative damage. AChE-IN-120 can be used for the research of Alzheimer's disease .
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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-107111A
CAS No.: 932373-86-9
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GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride 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-12355R
CAS No.: 1230487-00-9
Synonyms: BAF-312 (Standard)
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Siponimod (BAF-312) (Standard) is the analytical standard of Siponimod. This product is intended for research and analytical applications. Siponimod 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.
Cat. No.: HY-125577
CAS No.: 192756-07-3
Synonyms: RU-36384
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VRT-18858 (RU-36384), the active metabolite of Pralnacasan (HY-19676), is a potent interleukin-1β converting enzyme (ICE) inhibitor (Ki = 1.4 nM). VRT-18858 inhibits LPS (HY-D1056)-induced IL-1β release (IC50 = 0.42 µM) and S. aureus Cowan-induced IL-1β and IL-18 release (IC50=1.3 and 2.1 µM, respectively) in human peripheral blood mononuclear cells. VRT-18858 can be used for osteoarthritis research .
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 .
Cat. No.: HY-12355S
CAS No.: 2104759-32-0
Synonyms: BAF-312-d11
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-165478
CAS No.: 155651-56-2
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FCE 28260 is an orally active 4-azacyclic 5α-reductase (5αR) inhibitor. FCE 28260 exhibits IC₅₀ values for human 5αR type 1 and 5αR type 2 of 36 and 3.3 nM, respectively, and for human and rat prostates with IC₅₀ values of 16 and 15 nM, respectively. FCE 28260 simultaneously blocks the production of dihydrotestosterone (DHT) in the prostate and peripheral tissues. FCE 28260 can significantly inhibit the induction of prostatic and seminal vesicle hyperplasia by testosterone (T) in rat models, without inhibiting the growth of the prostate in DHT implantation models. FCE 28260 can be used for the studies DHT-dependent diseases such as benign prostatic hyperplasia (BPH) .
Cat. No.: HY-17609S
Synonyms: CR-845-d5; FE-202845-d5
Cat. No.: HY-17609S1
Synonyms: CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride
Cat. No.: HY-179164S
CAS No.: 287484-43-9
Choline- 15N chloride is the 15N-labeled Choline chloride (HY-B1337). Choline chloride is an orally active methylxanthine derivative. Choline chloride exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline chloride relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. Choline chloride modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline chloride is used in studies of bronchospasm, nocturnal asthma, and chronic asthma .
Cat. No.: HY-183206
CAS No.: 149455-36-7
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UR 8225 is an orally active ATP-sensitive K + channel activator with vasodilator, smooth muscle relaxant, antihypertensive, and bronchodilator activities. UR 8225 induces membrane hyperpolarization by increasing outward K + conductance and reduces Ca 2+ influx through voltage-gated L-type Ca 2+ channels. UR 8225 reduces total peripheral vascular resistance, shortens cardiac action potential duration, inhibits agonist-induced Ca 2+ influx, and stimulates renin release. UR 8225 induces reflex tachycardia but lacks β-adrenergic receptor blocking activity. UR 8225 is widely applicable to research in fields related to hypertension, myocardial ischemia, ventricular fibrillation, and other conditions .
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Cat. No.: HY-B1337S2
CAS No.: 3035513-80-2
Choline-d6 chloride is the d6-labeled Choline chloride (HY-B1337). Choline chloride is an orally active methylxanthine derivative. Choline chloride exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline chloride relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. Choline chloride modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline chloride is used in studies of bronchospasm, nocturnal asthma, and chronic asthma .
Cat. No.: HY-B1337S3
CAS No.: 352438-97-2
Choline-d13 chloride is the d13-labeled Choline chloride (HY-B1337). Choline chloride is an orally active methylxanthine derivative. Choline chloride exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline chloride relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. Choline chloride modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline chloride is used in studies of bronchospasm, nocturnal asthma, and chronic asthma .
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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
