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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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₄₄H₅₈N₈O₂S₂·4HCl·nH₂O

Products

Catalogue NumberPackaging Qty/Pack
5.33299.0001 Glass bottle 10 mg
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
Catalogue Number GTIN
5.33299.0001 04055977281538

Documentation

Gαq G Protein Inhibitor, BIM-46187 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
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.
Data Sheet

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.