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BIM-46187 (hydrochloride)

Catalog No.GC49300

An inhibitor of heterotrimeric G-protein signaling

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BIM-46187 (hydrochloride) Chemical Structure

Cas No.: 2489449-03-6

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1 mg
$67.00
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5 mg
$235.00
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10 mg
$369.00
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25 mg
$1,350.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

BIM-46187 is an inhibitor of heterotrimeric G-protein signaling.1,2 It inhibits signaling through Gαi, Gαs, and Gαq in MZ7 cells but selectively inhibits Gαq in HEK293 and CHO cells, indicating cell-dependent inhibition.1 BIM-46187 (0.1-1 mg/kg) increases the paw withdrawal threshold to a mechanical stimulus in a rat model of carrageenan-induced hyperalgesia.3 It also reduces mechanical hyperalgesia in a rat model of neuropathic pain induced by chronic constriction injury (CCI) when administered at doses ranging from 0.3 to 3 mg/kg.

1.Schmitz, A.-L., Schrage, R., Gaffal, E., et al.A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformationChem. Biol.21(7)890-902(2014) 2.Zhang, H., Nielsen, A.L., and StrØmgaard, K.Recent achievements in developing selective Gq inhibitorsMed. Res. Rev.40(1)135-157(2019) 3.Favre-Guilmard, C., Zeroual-Hide, H., Soulard, C., et al.The novel inhibitor of the heterotrimeric G-protein complex, BIM-46187, elicits anti-hyperalgesic properties and synergizes with morphineEur. J. Pharmacol.594(1-3)70-76(2008)

Chemical Properties

Cas No. 2489449-03-6 SDF
Canonical SMILES O=C(N1[C@H](C2=NC(C3=CC=CC=C3)=CN2CC1)CC4CCCCC4)[C@@H](N)CSSC[C@H](N)C(N5CCN6C([C@@H]5CC7CCCCC7)=NC(C8=CC=CC=C8)=C6)=O.Cl.Cl.Cl.Cl
Formula C44H58N8O2S2·4HCl M.Wt 941
Solubility DMF: 30 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.0627 mL 5.3135 mL 10.627 mL
5 mM 0.2125 mL 1.0627 mL 2.1254 mL
10 mM 0.1063 mL 0.5313 mL 1.0627 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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