500527 APETx2, Anthopleura elegantissima, Recombinant, E. coli - Calbiochem

500527
Le prix n'a pas pu être récupéré
La quantité minimale doit être un multiple de
À la validation de la commande Plus d'informations
Vous avez sauvegardé ()
 
Demander le prix
Disponibilité limitéeDisponibilité limitée
En stock 
Interrompu(e)
Disponible en quantités limitées
Disponibilité à confirmer
    Pour le restant : Nous vous tiendrons informé
      Pour le restant : Nous vous tiendrons informé
      Nous vous tiendrons informé
      Contacter le Service Clients
      Contact Customer Service
      Voir les Prix & la Disponibilité

      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      Empirical Formula
      C₁₉₆H₂₈₀N₅₄O₆₁S₆

      Prix & Disponibilité

      Référence DisponibilitéConditionnement Qté Prix Quantité
      5005270001
      Récupération des données relatives à la disponibilité...
      Disponibilité limitéeDisponibilité limitée
      En stock 
      Interrompu(e)
      Disponible en quantités limitées
      Disponibilité à confirmer
        Pour le restant : Nous vous tiendrons informé
          Pour le restant : Nous vous tiendrons informé
          Nous vous tiendrons informé
          Contacter le Service Clients
          Contact Customer Service

          Flacon en verre 100 μg
          Prix en cours de récupération
          Le prix n'a pas pu être récupéré
          La quantité minimale doit être un multiple de
          À la validation de la commande Plus d'informations
          Vous avez sauvegardé ()
           
          Demander le prix
          Description
          OverviewOriginally isolated from sea anemone Anthopleura elegantissima, the 42 amino-acid toxin APETx2 is shown to block acidification-induced activation of homotrimeric acid-sensing ion channel composed of rat or human ASIC3, but not rat ASIC1a, ASIC1b, or ASIC2a, in a reversible manner. APETx2 is also shown to inhibit the Na+-dependent, alkalization-induced "nonconventional" channel activity seen in human, but not rat, ASIC3. APETx2 in vivo efficacy is demonstrated in various rat pain induction models (100 µL 2.2 µM APETx2 via i.m. injection). Reported to display much reduced potency against Kv3.4 and little or no effect toward hERG, Kv2.2, Kv3.1, Kv4.2, or Kv4.3 channel activity.
          Catalogue Number500527
          Brand Family Calbiochem®
          SynonymsAcid-Sensing Ion Channel 3 Blocker, ASIC3 Channel Blocker
          References
          ReferencesDelaunay, A., et al. 2012. Proc. Natl. Acad. Sci. 109, 13124.
          Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
          Karczewski, J., et al. 2010. Br J Pharmacol. 161, 950.
          Chagot, B., et al. 2005. Protein Sci. 14, 2003.
          Diochot, S., et al. 2004. EMBO J. 23, 1516.
          Product Information
          FormLyophilized powder
          FormulationSupplied as a trifluoroacetate salt.
          Hill FormulaC₁₉₆H₂₈₀N₅₄O₆₁S₆
          Chemical formulaC₁₉₆H₂₈₀N₅₄O₆₁S₆
          ReversibleY
          Quality LevelMQ100
          Applications
          Biological Information
          Primary TargetASIC3
          Primary Target IC<sub>50</sub>63 nM
          Purity≥95% by HPLC
          Physicochemical Information
          Peptide SequenceH-Gly-Thr-Ala-Cys⁴-Ser-Cys⁶-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys²⁰-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys³⁰-Arg-Tyr-Phe-Leu-Gly-Thr-Cys³⁷-Cys³⁸-Thr-Pro-Ala-Asp-OH (disulfide bonds: 4 → 37, 6 → 30, 20 → 38)
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Shipped with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage -20°C
          Protect from Light Protect from light
          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

          Documentation

          APETx2, Anthopleura elegantissima, Recombinant, E. coli - Calbiochem FDS

          Titre

          Fiche de données de sécurité des matériaux (FDS) 

          Références bibliographiques

          Aperçu de la référence bibliographique
          Delaunay, A., et al. 2012. Proc. Natl. Acad. Sci. 109, 13124.
          Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
          Karczewski, J., et al. 2010. Br J Pharmacol. 161, 950.
          Chagot, B., et al. 2005. Protein Sci. 14, 2003.
          Diochot, S., et al. 2004. EMBO J. 23, 1516.
          Fiche technique

          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.

          Revision17-July-2013 JSW
          SynonymsAcid-Sensing Ion Channel 3 Blocker, ASIC3 Channel Blocker
          DescriptionOriginally isolated from sea anemone Anthopleura elegantissima, the 42 amino-acid toxin APETx2 is shown to block acidification-induced activation of homotrimeric acid-sensing ion channel composed of rat or human ASIC3 (IC50 against pH 7.4 to 6 ramping-induced transient current = 63 nM and 175 nM by whole-cell patch-clamp using COS cells expressing respective channel), but not rat ASIC1a, ASIC1b, or ASIC2a, in a reversible manner, presumably via its N-terminus interaction with type I β turn that connects β-strands I&II in the ASIC3 extracellular β-ball region. In addition to acidification-induced classical transient current, APETx2 is also shown to inhibit the Na+-dependent, alkalization-induced nonconventional channel activity seen in human, but not rat, ASIC3 (complete inhibition by 1 µM APETx3; pH 8.0). APETx2 in vivo efficacy is demonstrated in various rat pain induction models, including acid- (via calf i.m. injection of 100 µL pH 4.0 saline on day 1&5) induced mechanical hypersensitivity (pain withdrawal threshold = 76% and 24% of control rats with or without 100 µL 2.2 µM APETx2 i.m. injection prior to the second pH 4.0 saline injection). Although structurally related to known K+ channel modulators APETx1 and BDS-1/II, APETx2 is reported to display much reduced potency against Kv3.4 (38% inhibition by 3 µM APETx2) and little or no effect toward hERG, Kv2.2, Kv3.1, Kv4.2, or Kv4.3 channel activity.
          FormLyophilized powder
          FormulationSupplied as a trifluoroacetate salt.
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₉₆H₂₈₀N₅₄O₆₁S₆
          Peptide SequenceH-Gly-Thr-Ala-Cys⁴-Ser-Cys⁶-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys²⁰-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys³⁰-Arg-Tyr-Phe-Leu-Gly-Thr-Cys³⁷-Cys³⁸-Thr-Pro-Ala-Asp-OH (disulfide bonds: 4 → 37, 6 → 30, 20 → 38)
          Purity≥95% by HPLC
          SolubilityAqueous buffer
          Storage -20°C
          Protect from light
          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
          ReferencesDelaunay, A., et al. 2012. Proc. Natl. Acad. Sci. 109, 13124.
          Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
          Karczewski, J., et al. 2010. Br J Pharmacol. 161, 950.
          Chagot, B., et al. 2005. Protein Sci. 14, 2003.
          Diochot, S., et al. 2004. EMBO J. 23, 1516.