Velusetrag - Moligand™, 10mM in DMSO , CAS No.866933-46-2

CAS: 866933-46-2 Cat. No.: V656477 Formula: C₂₅H₃₆N₄O₅S Peso molecolare: 504.64

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT 4 receptor (5-HT4R) , with a pK i of 7.7. Velusetrag exhibits no affinity (K i >10 μM) for 5-HT 2A and 5-HT 2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease

In Vitro

Velusetrag (10 pM-100 μM) concentration-dependently increases the cAMP in HEK-293 cells stably transfected with the h5-HT4(c) receptor, with a pEC 50 of 8.3. Velusetrag (100 pM-1 μM) produces concentration-dependent contraction of the guinea pig colonic longitudinal muscle/myenteric plexus (LMMP), with a pEC 50 of 7.9. Velusetrag (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC 50 of 7.9. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Velusetrag (3 mg/kg; a single i.p.) significantly improves the facilitation of contextual fear extinction in PD mice. Velusetrag (3 mg/kg; a single i.p.) increases hippocampal cAMP levels in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice. Velusetrag (0.003-3 mg/kg; a single s.c.) increases colonic transit in a dose-dependent manner and reduces the time taken for excretion of the dye in guinea pigs. Velusetrag (0.003-1 mg/kg; a single i.v.) dose-dependently increases inter-crystal distance, consistent with relaxation of the oesophagus in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6 mice (7-8 weeks old) were injected with MPTPDosage: 3 mg/kg Administration: A single i.p. Result: Improved facilitation of contextual fear extinction. Did not improve the impaired rotarod performance in PD mice.

IC50& Target:5-HT 4 Receptor 7.7 (pKi)

Specifications

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT 4 receptor (5-HT4R) , with a pK i of 7.7. Velusetrag exhibits no affinity (K i >10 μM) for 5-HT 2A and 5-HT 2B receptors. Velusetrag can be used for the research of g

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

AGONIST

Proprietà del prodotto

• ALogP: 1.7

Nomi e identificatori

• Isomeri SMILES: CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3C[C@H]4CC[C@@H](C3)N4C[C@H](CN(C)S(=O)(=O)C)O
• CAS alternativo: 866933-46-2;866933-51-9
• Termini MeSH: 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid ((1S,3R,5R)-8-((R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl)-8-aza-bicyclo(3.2.1)oct-3-yl)amide;TD-5108;TD5108;velusetrag
• Peso molecolare: 504.64

Obiettivi associati (umani)

HTR4 Tclin 5-hydroxytryptamine receptor 4 (0 Activities)

Discover Target: HTR4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)