5.33299
Gαq G Protein Inhibitor, BIM-46187
別名:
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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この商品について
実験式（ヒル表記法）:
C44H58N8O2S2 · 4HCl · xH2O
分子量:
940.96 (anhydrous basis)
NACRES:
NA.77
UNSPSC Code:
12352202
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
assay
≥98% (HPLC)
Quality Segment
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)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
5332990001: + 5332990002:
jan
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。