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Desformylflustrabromine hydrochloride

CAS# 951322-11-5

Desformylflustrabromine hydrochloride

Catalog No. BCC7651----Order now to get a substantial discount!

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Chemical structure

Desformylflustrabromine hydrochloride

3D structure

Chemical Properties of Desformylflustrabromine hydrochloride

Cas No. 951322-11-5 SDF Download SDF
PubChem ID 56675778 Appearance Powder
Formula C16H22BrClN2 M.Wt 357.72
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 10 mM in water with gentle warming
Chemical Name 2-[6-bromo-2-(2-methylbut-3-en-2-yl)-1H-indol-3-yl]-N-methylethanamine;hydrochloride
SMILES CC(C)(C=C)C1=C(C2=C(N1)C=C(C=C2)Br)CCNC.Cl
Standard InChIKey GEZWEAPBLKXKGN-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H21BrN2.ClH/c1-5-16(2,3)15-13(8-9-18-4)12-7-6-11(17)10-14(12)19-15;/h5-7,10,18-19H,1,8-9H2,2-4H3;1H
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 Desformylflustrabromine hydrochloride

DescriptionPositive allosteric modulator of nicotinic α4β2 receptors; selectively increases the ionic current through α4β2 in the presence of ACh. Displays 14.7-fold selectivity for α4β2 over homomeric (α7) receptors. Moderately cytotoxic in HCT-116 cells. Also inhibits human muscle (αβεδ) and Torpedo (αβγδ) nAChRs (IC50 values are 1.0 and 0.1 μM, respectively) by binding in the ion channel.

Desformylflustrabromine hydrochloride Dilution Calculator

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Preparing Stock Solutions of Desformylflustrabromine hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7955 mL 13.9774 mL 27.9548 mL 55.9097 mL 69.8871 mL
5 mM 0.5591 mL 2.7955 mL 5.591 mL 11.1819 mL 13.9774 mL
10 mM 0.2795 mL 1.3977 mL 2.7955 mL 5.591 mL 6.9887 mL
50 mM 0.0559 mL 0.2795 mL 0.5591 mL 1.1182 mL 1.3977 mL
100 mM 0.028 mL 0.1398 mL 0.2795 mL 0.5591 mL 0.6989 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 Desformylflustrabromine hydrochloride

Nicotine facilitates nicotinic acetylcholine receptor targeting to mitochondria but makes them less susceptible to selective ligands.[Pubmed:28700952]

Neurosci Lett. 2017 Aug 24;656:43-50.

Several nicotinic acetylcholine receptor (nAChR) subtypes are expressed in mitochondria to regulate the internal pathway of apoptosis in ion channel-independent manner. However, the mechanisms of nAChR activation in mitochondria and targeting to mitochondria are still unknown. Nicotine has been shown to favor nAChR pentamer assembly, folding, and maturation on the way of biosynthesis. The idea of the present work was to determine whether nicotine affects the content, glycosylation, and function of mitochondrial nAChRs. Experiments were performed in isolated liver mitochondria from mice, that either consumed or not nicotine with the drinking water (200muL/L) for 7days. Mitochondria detergent lysates were studied by sandwich or lectin ELISA for the presence and carbohydrate composition of different nAChR subunits. Intact mitochondria were examined by flow cytometry for the binding of fluorescently labeled alpha-cobratoxin and were tested in functional assay of cytochrome c release under the effect of either Ca(2+) or wortmannin in the presence or absence of nAChR-selective ligands, including PNU-282987 (1nM), dihydro-beta-erythroidine (DhbetaE, 1muM), PNU-120596 (0.3, 3, or 10muM) and Desformylflustrabromine hydrochloride (dFBr, 0.001, 0.3, or 1muM). It was found that nicotine consumption increased the ratio of mitochondrial vs non-mitochondrial nAChRs in the liver, enhanced fucosylation of mitochondrial nAChRs, but prevented the binding of alpha-cobratoxin and the cytochrome c release-attenuating effects of nAChR-specific agonists, antagonists, or positive allosteric modulators. It is concluded that nicotine consumption in vivo favors nAChR glycosylation and trafficking to mitochondria but makes them less susceptible to the effects of specific ligands.

Desformylflustrabromine (dFBr) and [3H]dFBr-Labeled Binding Sites in a Nicotinic Acetylcholine Receptor.[Pubmed:25870334]

Mol Pharmacol. 2015 Jul;88(1):1-11.

Desformylflustrabromine (dFBr) is a positive allosteric modulator (PAM) of alpha4beta2 and alpha2beta2 nAChRs that, at concentrations >1 microM, also inhibits these receptors and alpha7 nAChRs. However, its interactions with muscle-type nAChRs have not been characterized, and the locations of its binding site(s) in any nAChR are not known. We report here that dFBr inhibits human muscle (alphabetaepsilondelta) and Torpedo (alphabetagammadelta) nAChR expressed in Xenopus oocytes with IC50 values of approximately 1 muM. dFBr also inhibited the equilibrium binding of ion channel blockers to Torpedo nAChRs with higher affinity in the nAChR desensitized state ([(3)H]phencyclidine; IC50 = 4 muM) than in the resting state ([(3)H]tetracaine; IC50 = 60 muM), whereas it bound with only very low affinity to the ACh binding sites ([(3)H]ACh, IC50 = 1 mM). Upon irradiation at 312 nm, [(3)H]dFBr photoincorporated into amino acids within the Torpedo nAChR ion channel with the efficiency of photoincorporation enhanced in the presence of agonist and the agonist-enhanced photolabeling inhibitable by phencyclidine. In the presence of agonist, [(3)H]dFBr also photolabeled amino acids in the nAChR extracellular domain within binding pockets identified previously for the nonselective nAChR PAMs galantamine and physostigmine at the canonical alpha-gamma interface containing the transmitter binding sites and at the noncanonical delta-beta subunit interface. These results establish that dFBr inhibits muscle-type nAChR by binding in the ion channel and that [(3)H]dFBr is a photoaffinity probe with broad amino acid side chain reactivity.

Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.[Pubmed:17604168]

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4855-60.

Desformylflustrabromine (dFBr; 1) and desformylflustrabromine-B (dFBr-B; 2) have been previously isolated from natural sources, and the former has been demonstrated to be a novel and selective positive allosteric modulator of alpha4beta2 nicotinic acetylcholine (nACh) receptors. The present study describes the synthesis of water-soluble salts of 1 and 2, and confirms and further investigates the actions of 1 and 2 using two-electrode voltage clamp recordings.

Description

Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.

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