FGIN-1-43

Potent, specific ligand for mitochondrial DBI receptor CAS# 145040-29-5

FGIN-1-43

Catalog No. BCC6739----Order now to get a substantial discount!

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FGIN-1-43: 5mg $81 In Stock
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Quality Control of FGIN-1-43

Number of papers citing our products

Chemical structure

FGIN-1-43

3D structure

Chemical Properties of FGIN-1-43

Cas No. 145040-29-5 SDF Download SDF
PubChem ID 3995234 Appearance Powder
Formula C28H36Cl2N2O M.Wt 487.51
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name 2-[5-chloro-2-(4-chlorophenyl)-1H-indol-3-yl]-N,N-dihexylacetamide
SMILES CCCCCCN(CCCCCC)C(=O)CC1=C(NC2=C1C=C(C=C2)Cl)C3=CC=C(C=C3)Cl
Standard InChIKey XTZUPNNVXIMWAR-UHFFFAOYSA-N
Standard InChI InChI=1S/C28H36Cl2N2O/c1-3-5-7-9-17-32(18-10-8-6-4-2)27(33)20-25-24-19-23(30)15-16-26(24)31-28(25)21-11-13-22(29)14-12-21/h11-16,19,31H,3-10,17-18,20H2,1-2H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of FGIN-1-43

DescriptionMost active of the 2-aryl-3-indoleacetamides; a new class of potent and specific ligands as probes for the mitochondial DBI receptor (peripheral benzodiazepine receptor).

FGIN-1-43 Dilution Calculator

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FGIN-1-43 Molarity Calculator

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Preparing Stock Solutions of FGIN-1-43

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0512 mL 10.2562 mL 20.5124 mL 41.0248 mL 51.281 mL
5 mM 0.4102 mL 2.0512 mL 4.1025 mL 8.205 mL 10.2562 mL
10 mM 0.2051 mL 1.0256 mL 2.0512 mL 4.1025 mL 5.1281 mL
50 mM 0.041 mL 0.2051 mL 0.4102 mL 0.8205 mL 1.0256 mL
100 mM 0.0205 mL 0.1026 mL 0.2051 mL 0.4102 mL 0.5128 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on FGIN-1-43

Synthesis and preliminary behavioural evaluation in mice of new 3-aryl-3-pyrrol-1-ylpropanamides, analogues of FGIN-1-27 and FGIN-1-43.[Pubmed:11732760]

J Pharm Pharmacol. 2001 Nov;53(11):1561-8.

The 2-aryl-3-indoleacetamides FGIN-1-27 and FGIN-1-43 have already been characterized in-vitro as potent and specific ligands for the mitochondrial DBI receptor. This affinity was associated with psychotropic properties in several rodent behavioural tasks (in particular anxiolytic action) via enhancement of GABA transmission through neurosteroid production. The synthesis of new 3-aryl-3-pyrrol-1-ylpropanamides 1a-i, analogues of FGIN-1-27 and FGIN-1-43, is described in four steps starting from the corresponding arylaldehydes. Preliminary evaluation of these compounds in behavioural studies (spontaneous locomotor activity and anxiolytic activity) in mice was also undertaken.

Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.[Pubmed:8411007]

J Med Chem. 1993 Oct 1;36(20):2908-20.

The mitochondrial DBI receptor complex (mDRC; previously called the peripheral benzodiazepine receptors) is linked to the production of neurosteroids such as pregnenolone sulfate, dehydroepiandrosterone sulfate, and others. In order to gain further information as to the function of the mDRC in the brain, we have constructed and tested both in vitro and in vivo a novel series of ligands, 2-arylindole-3-acetamides. The SAR studies detailed herein delineate some of the structural features required for high affinity binding to the mDRCs. In most cases the new ligands were prepared by use of the Fischer indole synthesis. Variations in the length and number of the alkyl groups on the amide nitrogen were probed together with the effects of halogen substituents on one or both of the aryl rings. Some ligands were also synthesized for study which represent conformationally constrained versions of the parent structure. Broad screening studies revealed these indoleacetamides to be highly selective for the mDRC, since they failed to bind with any significant affinity to other receptor systems. Some of the ligands were found to exhibit Ki values in the low nanomolar range for the mDRC as measured by the displacement of [3H]4'-chlorodiazepam. A subset of these ligands was also shown to stimulate pregnenolone formation from the mitochondria of C6-2B glioma cells with an EC50 of about 3 nM. In animal experiments ligands selected for further study were found to exhibit antineophobic effects, in spite of the fact that they exhibit no direct action on GABAA receptors. Consequently, it is postulated that these ligands owe their action to an indirect modulation of GABAA receptor function, presumably by stimulation of neurosteroid production and release from glial cells, followed by neurosteroid modulation of GABA's action on the chloride ion channel conductance of GABAA receptors.

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