Prucalopride - Moligand™, 10mM in DMSO , Serotonin 4 (5-HT4) receptor agonist, CAS No.179474-81-8, Serotonin 4 (5-HT4) receptor agonist

CAS: 179474-81-8 Cat. No.: P408108 Peso molecular: 367.87 Número EC: 878-837-3
Disponible para pedir
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Synonyms
R-93877 | 7-Benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
 ·  off list, applied to all prices below.
Size
Estado
Price
Qty
1ml
P408108-1ml
1

67,90US$

98,90US$
Guardar 31,00 US$ (31.34%)
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Descripción general

Information

Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for5-HT4Aand5-HT4Breceptor withKiof 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
In vitro

Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve.

In vivo

Complete bowel movements per week is 30.9% of those receiving 2 mg of Prucalopride and 28.4% of those receiving 4 mg of Prucalopride, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of Prucalopride and 46.6% of those receiving 4 mg of Prucalopride has an increase in the number of spontaneous, complete bowel movements of one or more per week, on average, as compared with 25.8% in the placebo group. Prucalopride (2 mg or 4 mg) significantly improves all other secondary efficacy end points, including patients\' satisfaction with their bowel function and treatment and their perception of the severity of their constipation symptoms. Prucalopride (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. Prucalopride (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying. Higher proportions of patients on prucalopride 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). Prucalopride also significantly improves secondary efficacy and quality of life endpoints, including the proportion of patients with an increase of one or more SCBM/week, evacuation completeness, perceived disease severity and treatment effectiveness and quality of life. Prucalopride alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon and by inhibiting contractile activity in the distal colon of fasted dogs. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment.
Cell Data

cell lines:A.E7 or Th17 cells

Concentrations:

Incubation Time:

Powder Purity:≥99%

Specifications

Sinónimos
R-93877 | 7-Benzofurancarboxamide, 4-amino-5-chloro-2, 3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-
Especificaciones y pureza
Moligand™, 10mM in DMSO
Mecanismos bioquímicos y fisiológicos
Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
Grado
Moligand™
Tipo de acción
AGONIST
Mecanismo de acción
Serotonin 4 (5-HT4) receptor agonist
Propiedades del producto
ALogP2
Nombres e identificadores
Isómeros SMILES COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
Peso molecular 367.87
Reaxy-Rn 8357099
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8357099&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Objetivos asociados (humanos)
HTR4 Tclin 5-hydroxytryptamine receptor 4 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HTR3A Tclin 5-hydroxytryptamine receptor 3A (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificados (CoA, COO, BSE/TSE y tabla de análisis)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propiedades químicas y físicas
SolubilidadSolubility (25°C) In vitro DMSO: 42 mg/mL (197.89 mM); Ethanol: 5 mg/mL (23.55 mM); Water: Insoluble;
Punto de fusión (°C)92 °C
Calculadoras de soluciones
Reseñas

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