An inhibitor of heterotrimeric G-protein signaling
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Product Categories

Product Type

Biochemicals

Research Area

Cell Biology
Cell Signaling
Neuroscience
Pain Research

BIM-46187 (hydrochloride)

Item No. 34531

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R,2′R)-3,3′-dithiobis[2-amino-1-[(8S)-8-(cyclohexylmethyl)-5,6-dihydro-2-phenylimidazo[1,2-a]pyrazin-7(8H)-yl]-1-propanone, tetrahydrochloride
CAS Number
2489449-03-6
Molecular Formula
C44H58N8O2S2 • 4HCl
Formula Weight
941.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
260 nm
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
InChi Code
InChI=1S/C44H58N8O2S2.4ClH/c45-35(43(53)51-23-21-49-27-37(33-17-9-3-10-18-33)47-41(49)39(51)25-31-13-5-1-6-14-31)29-55-56-30-36(46)44(54)52-24-22-50-28-38(34-19-11-4-12-20-34)48-42(50)40(52)26-32-15-7-2-8-16-32;;;;/h3-4,9-12,17-20,27-28,31-32,35-36,39-40H,1-2,5-8,13-16,21-26,29-30,45-46H2;4*1H/t35-,36-,39-,40-;;;;/m0..../s1
InChi Key
RKTRULIWGAJVGM-FPBFTDTKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $203

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    10 mg

    $324

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    25 mg

    $742

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    Product Description

    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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schmitz, A.-L., Schrage, R., Gaffal, E., et al. A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformation. Chem. Biol. 21(7), 890-902 (2014).

    2. Zhang, H., Nielsen, A.L., and Strømgaard, K. Recent achievements in developing selective Gq inhibitors. Med. 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 morphine. Eur. J. Pharmacol. 594(1-3), 70-76 (2008).