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532383 Donecopride Fumarate - Calbiochem

A cell permeable, highly potent, selective, and partial agonist of serotonin subtype 4 receptor (Ki= 10.4 nM). Also acts as a potent, mixed type, competitive inhibitor of AChE (IC₅₀ = 16 nM).

Donecopride Fumarate - Calbiochem: Ficha de datos de seguridad (MSDS o SDS), certificado de análisis y de calidad (CoA y CoQ), expedientes, folletos y otros documentos disponibles.

Sinónimos: 5-HT4R Agonist, AChE Inhibitor, MR31147, Serotonin receptor 5-HT4R agonist

Primary Target: 5-HT4R
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      Descripción

      Replacement Information

      Tabla espec. clave

      Empirical Formula
      C₂₂H₃₃ClN₂O₂·C₄H₄O₄·xH₂O
      Description
      Overview

      This product has been discontinued.



      A cell permeable, brain penetrating piperidin-4-yl-propanone compound that that acts as a highly potent, selective and partial agonist of serotonin subtype 4 receptor ((h)5-HT4R; Ki = 10.4 nM and 48% efficacy compared to 5-HT control). Also acts as a potent, mixed type, competitive inhibitor of acetylcholinesterase (IC50 = 16 nM for human AChE) and offers selectivity over butyrylcholinesterase (IC50 = 3.5 µM). With respect to 5-HT2BR, it behaves like an inverse agonist (Ki = 1.6 nM). Promotes sAPPα secretion in COS-7 cells transiently expressing 5-HT4R (EC50 = 11.3 nM) and is shown to have a precognitive effect in murine model where it significantly improves discrimination index (6.3 vs -.0.22 in control mice; 0.3 mg/kg).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.

      Catalogue Number532383
      Brand Family Calbiochem®
      Synonyms5-HT4R Agonist, AChE Inhibitor, MR31147, Serotonin receptor 5-HT4R agonist
      References
      ReferencesLecoutey, C., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3825.
      Product Information
      FormOff-white powder
      Hill FormulaC₂₂H₃₃ClN₂O₂·C₄H₄O₄·xH₂O
      Chemical formulaC₂₂H₃₃ClN₂O₂·C₄H₄O₄·xH₂O
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Target5-HT4R
      Primary Target K<sub>i</sub>10.4 nM
      Secondary targetAChE
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Número de referencia GTIN
      532383 0

      Documentation

      Donecopride Fumarate - Calbiochem Ficha datos de seguridad (MSDS)

      Título

      Ficha técnica de seguridad del material (MSDS) 

      Referencias bibliográficas

      Visión general referencias
      Lecoutey, C., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3825.

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      Licencias necesarias e Información técnica

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      Ficha técnica

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision15-March-2015 JSW
      Synonyms5-HT4R Agonist, AChE Inhibitor, MR31147, Serotonin receptor 5-HT4R agonist
      DescriptionA cell permeable, brain penetrating piperidin-4-yl-propanone compound that that acts as a highly potent, selective and partial agonist of serotonin subtype 4 receptor ((h)5-HT4R; Ki = 10.4 nM and 48% efficacy compared to 5-HT control). Also acts as a potent, mixed type, competitive inhibitor of acetylcholinesterase (IC50 = 16 nM for human AChE) and offers selectivity over butyrylcholinesterase (IC50 = 3.5 µM). With respect to 5-HT2BR, it behaves like an inverse agonist (Ki = 1.6 nM). Promotes sAPPα secretion in COS-7 cells transiently expressing 5-HT4R (EC50 = 11.3 nM) and is shown to have a precognitive effect in murine model where it significantly improves discrimination index (6.3 vs -.0.22 in control mice; 0.3 mg/kg).
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₃₃ClN₂O₂·C₄H₄O₄·xH₂O
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesLecoutey, C., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3825.