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Merck - 5.33299.0001 - Gq G Protein Inhibitor, BIM-46187 - Calbiochem

  • MFR SKU: 5.33299.0001
  • ITEM #: 11575553
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ITEM #: 11575553
A cell-permeable heterotrimeric G protein inhibitor that trap Gα q proteins in the empty pocket conformation. Exhibits analgesic effects and synergizes with morphine.
This listing is for 10 mg Glass bottle

Merck - 5.33299.0001 - G<sub>q</sub> G Protein Inhibitor, BIM-46187 - Calbiochem

  • Item #: 11575553
  • MFR SKU: 5.33299.0001
Technical Specs
  • Overview A cell-permeable tetrahydroimidazo[1, 2a]pyrazine dimer that directly binds to Gα subunit and inhibits heterotrimeric G protein signaling. Shown to selectively abolish Gα q signaling in HEK294 and CHO cells via trapping Gα q 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 Number 533299
  • Brand Family Calbiochem®
  • Synonyms (S, 2R, 2R)-3, 3-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
  • Gα q G Protein Inhibitor, BIM-46187
  • References 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.
  • Form Off-white solid
  • Formulation Supplied as a HCl salt.
  • Hill Formula CHNOS· 4HCl·nHO
  • Chemical formula CHNOS· 4HCl·nHO
  • Hygroscopic Hygroscopic
  • Reversible Y
  • Quality Level MQ100 50 $anchor_PDP_OverviewTab_Product_Biological_Info_Primary Target IC 50 " value=" Biological Information"
  • br> Primary Target IC<sub> 50</sub> 1 - 3 µ
  • Purity ≥ 98% by HPLC
  • Cell permeable Y
  • 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 Instructions Following reconstitution, aliquot and freeze (-20° C). Stock solutions are stable for up to 3 months at -20° C.
  • Packaged under inert gas Packaged under inert gas
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