Name: Prucalopride
Brand: Selleck Chemicals
SKU: S2875
Rating: 5 (5 reviews)

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Control de calidad (Quality Control)

Lote: Pureza: 99.97%

99.97

Dianas relacionadas	Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Otros 5-HT Receptor Inhibidores	Serotonin Hydrochloride (5-HT HCl) WAY-100635 Maleate Puerarin SB269970 HCl Ketanserin BRL-15572 Dihydrochloride RS-127445 Nuciferine Flopropione BRL-54443

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	367.87	Fórmula	C₁₈H₂₆ClN₃O₃	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	179474-81-8	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	R-93877			Smiles	COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 74 mg/mL (201.15 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 74 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	0.500mg/ml (1.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	5-HT4A 2.5 nM(Ki) 5-HT4B 8 nM(Ki)
In vitro	Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. This compound (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. It 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 this compound, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of this compound and 46.6% of those receiving 4 mg of it 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. This compound (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. It (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. This chemical (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying. Higher proportions of patients on this compound 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). It 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. This compound 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. It also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of this chemical, the first GMC generally occurres within the first half-hour after treatment.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/11438309/ [2] https://pubmed.ncbi.nlm.nih.gov/18509121/ [3] https://pubmed.ncbi.nlm.nih.gov/11159875/ [4] https://pubmed.ncbi.nlm.nih.gov/18987031/ [5] https://pubmed.ncbi.nlm.nih.gov/11696108/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT04838522	Recruiting	Chronic Constipation	Takeda\|UC San Diego Human Milk Research Biorepository	March 2 2022	--
NCT04429802	Completed	Gastrointestinal Motility Disorder\|Dyspepsia	Universitaire Ziekenhuizen KU Leuven	September 26 2013	Not Applicable
NCT01807000	Completed	Healthy	Shire\|Takeda	March 18 2013	Phase 1
NCT01692132	Withdrawn	Chronic Constipation	Janssen Pharmaceutica	February 2013	--
NCT03279341	Completed	Chronic Constipation	University Hospital Gasthuisberg	December 3 2012	Phase 4
NCT01117051	Terminated	Non-cancer Pain\|Opioid Induced Constipation	Shire\|Takeda	May 19 2010	Phase 3

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Prucalopride 5-HT Receptor agonist

Estructura química

Peso molecular: 367.87