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About This Item
Empirical Formula (Hill Notation):
C44H58N8O2S2 · 4HCl · xH2O
Molecular Weight:
940.96 (anhydrous basis)
UNSPSC Code:
12352202
NACRES:
NA.77
Assay
≥98% (HPLC)
Quality Level
form
solid
potency
1-3 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
off-white
solubility
water: 10 mg/mL
DMSO: 25 mg/mL
storage temp.
−20°C
General description
A 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.
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.
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Physical form
Supplied as a HCl salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
Ayoub, M. A., et al. 2009. J. Biol. Chem.284, 29136.
Favre-Guilmard, C., et al. 2008. Eur. J. Pharm.594, 70.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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