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61724
GBR-12909 Dihydrochloride
Activators & Inhibitors
Chemical Modulators

GBR-12909 Dihydrochloride #61724

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GBR-12909 Dihydrochloride: Image 1

Chemical structure of GBR-12909 Dihydrochloride.

Product Usage Information

GBR-12909 Dihydrochloride is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 10 mg of powder in 1.27 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 523.5 g/mol
Purity

>98%

Molecular Formula

C28H32F2N2O • 2HCl

CAS 67469-78-7
Solubility Soluble in DMSO at 30 mg/ml or water at 10 mg/ml both with slight warming.

Background

GBR-12909 Dihydrochloride is a highly selective synaptosomal dopamine uptake inhibitor (Ki = 1 nM), with a 100-fold stronger affinity for the dopamine uptake carrier protein than noradrenaline and serotonin (1). GBR-12909 Dihydrochloride has also been demonstrated to be a strong sigma receptor ligand in rat brain samples with an IC50 value of 48 nM (2). This small molecule is considered to be a high-affinity, long-acting dopamine transporter (DAT) inhibitor and in vivo models show that intravenous injection of GBR-12909 Dihydrochloride blocks dopamine uptake within 5 seconds, matching the temporal effect of cocaine, with longer-acting and less negative behavioral effects (3). The ability to regulate dopamine uptake makes GBR-12909 Dihydrochloride a compound of interest when studying substance abuse issues like alcohol and cocaine addiction (4,5).

  1. Andersen, P.H. (1989) Eur J Pharmacol 166, 493-504.
  2. Contreras, P.C. et al. (1990) Life Sci 47, PL133-7.
  3. Yorgason, J.T. et al. (2011) Neuroscience 182, 125-32.
  4. Tella, S.R. et al. (1996) J Neurosci 16, 7416-27.
  5. Kamdar, N.K. et al. (2007) Psychopharmacology (Berl) 192, 207-17.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
To Purchase # 61724S
Product # Size Price
61724S
10 mg $ 71