GBR-12935 HCl

• CAS: 67469-81-2
• Catalog Number: ACM67469812
• Category: Inhibitors
• Molecular Weight: 487.51
• Molecular Formula: C28H36Cl2N2O
• Description: GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. It was originally developed in its 3H radiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins. This has led to potential clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane (¹²³I) are now available for this application. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain.
• Synonyms: GBR-12935; GBR 12935; GBR12935
• IUPAC Name: 1-(2 (Diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride
• Canonical SMILES: [H]Cl.[H]Cl.N1(CCOC(C2=CC=CC=C2)C3=CC=CC=C3)CCN(CCCC4=CC=CC=C4)CC1
• InChI: InChI=1S/C28H34N2O.2ClH/c1-4-11-25(12-5-1)13-10-18-29-19-21-30(22-20-29)23-24-31-28(26-14-6-2-7-15-26)27-16-8-3-9-17-27;;/h1-9,11-12,14-17,28H,10,13,18-24H2;2*1H
• InChI Key: NQWRSILGEXNJIT-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Alternative CAS: 67469-81-2 (HCl); 76778-22-8 (free base); 1349767-56-1 (maleate)
• Biological Target: GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 68.98; H, 7.44; Cl, 14.54; N, 5.75; O, 3.28
• Exact Mass: 486.2205
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: GBR-12935 at 20 µM significantly inhibited tumoroid growth (Figure 5A,B). In contrast, the NET inhibitor nisoxetine did not alter tumoroid growth as compared to the untreated control. The MAT inhibitor amitriptyline significantly inhibited tumoroid growth, suggesting that DAT inhibition, but not NET inhibition, was required for tumoroid inhibition. GBR-12935 lowered the cancer cell viability of preformed tumoroids in a concentration-dependent manner (Figure 5C). Thus, DAT inhibition is a common mechanism by which Benz and GBR-12935 inhibit tumor growth.; Reference: Cancers (Basel). 2020 Feb 24;12(2):523. https://pubmed.ncbi.nlm.nih.gov/32102440/
• In Vivo Activity: As illustrated in Figure 7b, 20nM GBR12935 significantly and reversibly increased the frequency of sEPSCs recorded in VTA DA rat neurons (by 48±11%, n=6, p=0.01).; Reference: Neuropsychopharmacology. 2009 Jan;34(2):307-18. https://pubmed.ncbi.nlm.nih.gov/18596684/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).