Search Result
Results for "
5-HT4
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100170
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- HY-110094
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5-HT Receptor
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Neurological Disease
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BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors .
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- HY-14441
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5-HT Receptor
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Neurological Disease
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ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases .
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- HY-123695
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- HY-115774
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-
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- HY-103143A
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-
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- HY-103143
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5-HT Receptor
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Neurological Disease
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SDZ 205-557 hydrochloride is a selective 5-HT4 receptors antagonist. SDZ 205-557 hydrochloride can be used for neurological research .
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- HY-18138
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5-HT Receptor
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Neurological Disease
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PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex .
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- HY-100243
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Ticalopride
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5-HT Receptor
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Neurological Disease
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(+)-Norcisapride (Ticalopride) is a potent 5-HT4 agonist and a 5-HT3 antagonist. (+)-Norcisapride has activity in animals models of constipation .
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- HY-109065
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5-HT Receptor
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Others
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Minesapride is a partial agonist with a highly selective serotonin 4 (5-HT4) receptor. Minesapride enhances gastrointestinal peristalsis and colon transport by activating the 5-HT4 receptor. Minesapride increases bowel movements and suppresses visceral allergic reactions. Minesapride can be used in the study of constipation-type irritable bowel syndrome (IBS-C) .
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- HY-10457A
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TD-5108 hydrochloride
|
5-HT Receptor
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Neurological Disease
Metabolic Disease
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Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
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- HY-10457
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TD-5108
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5-HT Receptor
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Neurological Disease
Metabolic Disease
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Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .
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- HY-103134
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Others
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Inflammation/Immunology
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5-HT4 antagonist 3 hydrochloride is a highly selective 5-hydroxytryptamine receptor (5-HT4) antagonist. 5-HT4 antagonist 3 (hydrochloride) blocks muscarine receptors and sodium channels. 5-HT4 antagonist 3 (hydrochloride) can be used to evaluate function of 5-HT4 receptor .
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- HY-103137
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5-HT Receptor
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Neurological Disease
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Zacopride hydrochloride is a highly potent 5-HT3 receptor antagonist with Kis of 0.38 and 373 nM for 5-HT3 and 5-HT4 receptor, respectively. Zacopride hydrochloride is also a moderate IK1 channel agonist. Zacopride hydrochloride exerts significant antiarrhythmic and cardiac protective effects .
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- HY-14149
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R 51619; (±)-Cisaprid
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5-HT Receptor
Potassium Channel
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Neurological Disease
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Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .
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- HY-B2089
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- HY-14442
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- HY-14149A
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R 51619 monohydrate; (±)-Cisaprid monohydrate
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5-HT Receptor
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Neurological Disease
Metabolic Disease
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Cisapride monohydrate is an orally and potent 5-HT4 receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .
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- HY-14149R
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5-HT Receptor
Potassium Channel
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Neurological Disease
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Cisapride (Standard) is the analytical standard of Cisapride. This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .
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- HY-101668
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- HY-101341
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5-HT Receptor
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Neurological Disease
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RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
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- HY-B2089R
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
Metabolic Disease
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Cinitapride (Standard) is the analytical standard of Cinitapride. This product is intended for research and analytical applications. Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a 5-HT2 and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .
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- HY-15574A
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- HY-15574
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- HY-123747
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- HY-123747A
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- HY-19927A
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5-HT Receptor
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Neurological Disease
Endocrinology
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DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
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- HY-14152
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5-HT Receptor
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Cancer
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Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
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- HY-103108
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5-HT Receptor
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Metabolic Disease
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CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect .
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- HY-162591
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- HY-101222
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
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- HY-101638
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(±)-FK1052
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5-HT Receptor
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Neurological Disease
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(±)-Fabesetron hydrochloride ((±)-FK1052) is the racemate of Fabesetron hydrochloride, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist .
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- HY-121826
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- HY-102057
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TD-8954
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5-HT Receptor
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Others
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Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
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- HY-U00373
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- HY-101638A
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(±)-FK1052 free base
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5-HT Receptor
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Neurological Disease
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(±)-Fabesetron ((±)-FK1052 free base) is the racemate of Fabesetron, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist .
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- HY-16729A
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YKP10811 hydrochloride
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5-HT Receptor
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Inflammation/Immunology
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Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility .
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- HY-117574
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5-HT Receptor
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Cardiovascular Disease
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SB 207710 is a highly selective antagonist of the 5-HT4 receptor that has been shown to effectively block the positive inotropic effect induced by serotonin in human right atrial appendage preparations .
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- HY-B0189S1
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- HY-B0189A
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TAK-370 citrate; AS-4370 citrate
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5-HT Receptor
Potassium Channel
Cytochrome P450
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Neurological Disease
Cancer
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Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
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- HY-124381
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Others
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Others
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ML10375 is a compound that modulates 5-HT4 and 5-HT2 receptors, affects gap junction coupling in rat atrial myocytes, and regulates intracellular cAMP concentration and L-type calcium current.
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- HY-148846
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Drug Metabolite
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Metabolic Disease
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Mosapride N-Oxide is a major active metabolite of Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
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- HY-105201A
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FK1052
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5-HT Receptor
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Neurological Disease
Cancer
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Fabesetron (FK1052) hydrochloride is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron hydrochloride can be used in the study for both acute and delayed emesis induced by cancer chemotherapy .
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- HY-105201
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FK1052 free base
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5-HT Receptor
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Neurological Disease
Cancer
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Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy .
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- HY-128386
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- HY-116565
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SUVN-D4010
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5-HT Receptor
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Neurological Disease
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Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
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- HY-U00121
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5-HT Receptor
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Metabolic Disease
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Lintopride, a benzamide, is a potent 5HT-4 antagonist with moderate 5HT-3 antagonist properties. Lintopride increases gastric emptying, stimulates antral and duodenal motility and accelerates intestinal transit in animal. Lintopride significantly increases the lower oesophageal sphincter (LOS) basal tone .
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- HY-U00121A
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5-HT Receptor
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Metabolic Disease
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Lintopride hydrochloride, a benzamide, is a potent 5HT-4 antagonist with moderate 5HT-3 antagonist properties. Lintopride hydrochloride increases gastric emptying, stimulates antral and duodenal motility and accelerates intestinal transit in animal. Lintopride hydrochloride significantly increases the lower oesophageal sphincter (LOS) basal tone .
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- HY-14147
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BRL 24924
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5-HT Receptor
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Metabolic Disease
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Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist . Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study .
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- HY-116565A
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SUVN-D4010 free base
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5-HT Receptor
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Neurological Disease
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Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .
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- HY-101172
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EP-A-501322
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5-HT Receptor
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Cardiovascular Disease
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RS 23597-190 (EP-A-501322) is a high affinity and selective 5-HT4 receptor antagonist. RS 23597-190 inhibits 5-HT (HY-B1473A)-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .
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- HY-44132
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RS 42358-197
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5-HT Receptor
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Neurological Disease
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Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors .
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- HY-14153AS
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SDZ-HTF-919-13C,d3; HTF-919-13C,d3
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Isotope-Labeled Compounds
5-HT Receptor
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Neurological Disease
Metabolic Disease
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Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
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- HY-18137
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5-HT Receptor
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Neurological Disease
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PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .
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- HY-14147A
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(S)-BRL 24924
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5-HT Receptor
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Metabolic Disease
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(S)-Renzapride ((S)-BRL 24924) is the isomer of HY-14147 Renzapride. Renzapride is a 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride also is a 5HT2b and 5HT3 receptor antagonist. Renzapride can be used for constipation predominant irritable bowel syndrome (C-IBS) study .
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- HY-101653
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- HY-14148
-
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Others
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Neurological Disease
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Renzapride hydrochloride is a benzamide that inhibits irritable bowel syndrome and has antagonistic activity at 5-HT(3) receptors and agonistic activity at 5-HT(4) receptors. Renzapride hydrochloride also exhibits antagonistic activity at 5-HT(2B) receptors and has a certain affinity for 5-HT(2A) and 5-HT(2C) receptors .
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- HY-160921
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SL65.0155 free base
|
5-HT Receptor
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Neurological Disease
|
Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a Ki of 0.6 nM for 5-HT4 receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models .
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- HY-12694
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R-108512
|
5-HT Receptor
Apoptosis
Autophagy
|
Metabolic Disease
Cancer
|
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
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- HY-101343
-
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5-HT Receptor
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Neurological Disease
|
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
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- HY-10564
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MCI-9042
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5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
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- HY-10564S
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MCI-9042-d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
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- HY-121249
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SL65.0155
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5-HT Receptor
|
Neurological Disease
|
Capeserod hydrochloride (SL65.0155) is a 5-HT4(e) receptor partial agonist (Ki=0.6 nM) with potent cognitive enhancing properties. Capeserod hydrochloride acts as a partial agonist in cells expressing 5-HT4(b) and 5-HT4(e) splice variants, stimulating cAMP production with IC50 values ??of 244 and 29 nM, respectively. Capeserod hydrochloride is used in the study of memory impairment and dementia .
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- HY-B0189
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TAK-370; AS-4370
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5-HT Receptor
Cytochrome P450
Potassium Channel
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Neurological Disease
Cancer
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Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
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- HY-116266
-
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Others
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Others
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RS 67333 is a 5-HT4R agonist with stress-preventive activity. RS 67333 attenuates stress-induced body weight changes and prevents depression- and anxiety-like behaviors in two mouse strains tested in different stress models.
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- HY-103146
-
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5-HT Receptor
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Neurological Disease
|
GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction .
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- HY-14151
-
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5-HT Receptor
Apoptosis
Autophagy
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Neurological Disease
Cancer
|
Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
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- HY-14151R
-
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5-HT Receptor
Apoptosis
Autophagy
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Neurological Disease
Cancer
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Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
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- HY-103152
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- HY-14153
-
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5-HT Receptor
Apoptosis
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Metabolic Disease
Cancer
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Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
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- HY-14153A
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SDZ-HTF-919; HTF-919
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5-HT Receptor
Apoptosis
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Neurological Disease
Metabolic Disease
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Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
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- HY-14153S
-
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5-HT Receptor
Apoptosis
Isotope-Labeled Compounds
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Metabolic Disease
Cancer
|
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
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- HY-134807
-
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P2X Receptor
5-HT Receptor
Autophagy
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Cancer
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Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
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- HY-W015169
-
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- HY-W015169A
-
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5-HT Receptor
Endogenous Metabolite
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Neurological Disease
Cancer
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5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0189S1
-
|
Mosapride-d5 is the deuterium labeled Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
|
-
-
- HY-14153AS
-
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Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
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- HY-10564S
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Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
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- HY-14153S
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Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
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