5.33299
Gαq G Protein Inhibitor, BIM-46187
Synonym(s):
Gαq G Protein Inhibitor, BIM-46187, (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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About This Item
Empirical Formula (Hill Notation):
C44H58N8O2S2 · 4HCl · xH2O
Molecular Weight:
940.96 (anhydrous basis)
NACRES:
NA.77
UNSPSC Code:
12352202
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
新产品
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Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 5332990001 | 04055977281538 |