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5.33299

Gα_q G Protein Inhibitor, BIM-46187

Name: Gα<sub>q</sub> G Protein Inhibitor, BIM-46187
Brand: MM

别名:

Gα_q 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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关于此项目

经验公式（希尔记法）:

C₄₄H₅₈N₈O₂S₂ · 4HCl · xH₂O

分子量:

940.96 (anhydrous basis)

NACRES:

NA.77

UNSPSC Code:

12352202

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, desiccated (hygroscopic), protect from light

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属性

assay

≥98% (HPLC)

Quality Level

100

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

说明

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 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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c