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533299 Gαq G Protein Inhibitor, BIM-46187 - Calbiochem

A cell-permeable heterotrimeric G protein inhibitor that trap Gαq proteins in the empty pocket conformation. Exhibits analgesic effects and synergizes with morphine.

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Synonyme: (S,2R,2ʹR)-3,3ʹ-Disulfanediylbis(2-amino-1-((S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)propan-1-one) Tetrahydrochloride, 4HCl, BIM46187, G Protein Inhibitor, BIM-46187

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533299
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Übersicht

Replacement Information

Key Spec Table

Empirical Formula
C₄₄H₅₈N₈O₂S₂·4HCl·nH₂O

Preis & Verfügbarkeit

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      		 Glasflasche 10 mg
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      Description
      OverviewA cell-permeable tetrahydroimidazo[1,2a]pyrazine dimer that directly binds to Gα subunit and inhibits heterotrimeric G protein signaling. Shown to selectively abolish Gαq signaling in HEK294 and CHO cells via trapping Gαq in the empty pocket conformation by permitting GDP exit but interdicting GTP entry. In addition, elicits a dose-dependent analgesic effect in carrageenan-induced hyperalgesia (0.1-1 mg/kg, i.v.) and in a chronic constriction injury mouse model (0.3-3 mg/kg, i.v.), with synergistic effect when co-administered with morphine.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533299
      Brand Family Calbiochem®
      Synonyms(S,2R,2ʹR)-3,3ʹ-Disulfanediylbis(2-amino-1-((S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)propan-1-one) Tetrahydrochloride, 4HCl, BIM46187, G Protein Inhibitor, BIM-46187
      DescriptionGαq G Protein Inhibitor, BIM-46187
      References
      ReferencesSchmitz, A. et al. 1999. Chem. & Biol. 21, 890.
      Ayoub, M. A., et al. 2009. J. Biol. Chem. 284, 29136.
      Favre-Guilmard, C., et al. 2008. Eur. J. Pharm. 594, 70.
      Product Information
      FormOff-white solid
      FormulationSupplied as a HCl salt.
      Hill FormulaC₄₄H₅₈N₈O₂S₂·4HCl·nH₂O
      Chemical formulaC₄₄H₅₈N₈O₂S₂·4HCl·nH₂O
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Target IC<sub>50</sub>1 - 3 µ
      Purity≥98% 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
      Bestellnummer GTIN
      5332990001 04055977281538

      Documentation

      Gαq G Protein Inhibitor, BIM-46187 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Schmitz, A. et al. 1999. Chem. & Biol. 21, 890.
      Ayoub, M. A., et al. 2009. J. Biol. Chem. 284, 29136.
      Favre-Guilmard, C., et al. 2008. Eur. J. Pharm. 594, 70.
      Datenblatt

      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.

      Revision19-November-2016 JSW
      Synonyms(S,2R,2ʹR)-3,3ʹ-Disulfanediylbis(2-amino-1-((S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)propan-1-one) Tetrahydrochloride, 4HCl, BIM46187, G Protein Inhibitor, BIM-46187
      DescriptionA cell-permeable tetrahydroimidazo[1,2a]pyrazine dimer that directly binds to Gα subunit and inhibits heterotrimeric G protein signaling. Shown to selectively abolish Gαq signaling in HEK294 and CHO cells via trapping Gαq in the empty pocket conformation by permitting GDP exit but interdicting GTP entry. In addition, elicits a dose-dependent analgesic effect in carrageenan-induced hyperalgesia (0.1-1 mg/kg, i.v.) and in a chronic constriction injury mouse model (0.3-3 mg/kg, i.v.), with synergistic effect when co-administered with morphine.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      FormOff-white solid
      FormulationSupplied as a HCl salt.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₄₄H₅₈N₈O₂S₂·4HCl·nH₂O
      Purity≥98% by HPLC
      SolubilityDMSO (25 mg/ml) or H₂O (10 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
      ReferencesSchmitz, A. et al. 1999. Chem. & Biol. 21, 890.
      Ayoub, M. A., et al. 2009. J. Biol. Chem. 284, 29136.
      Favre-Guilmard, C., et al. 2008. Eur. J. Pharm. 594, 70.