2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Desformylflustrabromine hydrochloride

Desformylflustrabromine hydrochloride  (Synonyms: Deformylflustrabromine hydrochloride; dFBr hydrochloride)

Cat. No.: HY-107675 Purity: 99.77%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Desformylflustrabromine hydrochloride Chemical Structure

Desformylflustrabromine hydrochloride Chemical Structure

CAS No. : 951322-11-5

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Based on 1 publication(s) in Google Scholar

Desformylflustrabromine hydrochloride Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

α4β2 nAChR
In Vitro

Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48[1]. ACh-induced currents are potentiated and inhibited by Desformylflustrabromine hydrochloride in the high sensitivity (HS) and low sensitivity (LS) isoform preparations, although Desformylflustrabromine hydrochloride displays a higher potency on the LS isoform (pEC50=6.4±0.2) compare with the HS isoform (pEC50=5.6±0.2). Desformylflustrabromine hydrochloride potentiates ACh-induced responses of wild-type receptors expressed using the HS isoform preparation maximally by 350±20%, which is similar to receptors expressed via the LS isoform preparation (350±30%)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Desformylflustrabromine hydrochloride Related Antibodies
Molecular Weight

357.72

Formula

C16H22BrClN2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CNCCC1=C(C(C)(C)C=C)NC2=CC(Br)=CC=C12.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 105 mg/mL (293.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 5 mg/mL (13.98 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7955 mL 13.9774 mL 27.9548 mL
5 mM 0.5591 mL 2.7955 mL 5.5910 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.77%

COA (247 KB) HNMR (189 KB) RP-HPLC (380 KB) LCMS (382 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[2]

Receptors expressed via the high sensitivity (HS) isoform preparation are evaluated for Desformylflustrabromine hydrochloride modulation by coapplication of 10 μM ACh with increasing concentrations of Desformylflustrabromine hydrochloride (0.001 to 100 μM). To compare responses from different oocytes, individual responses to Desformylflustrabromine hydrochloride application are normalized to the control responses elicited using either 10 or 100 μM ACh for receptors expressed by the HS or LS isoform preparations, respectively, for both wild-type and mutated receptors. Data are collected from at least four replicate experiments using oocytes obtained from at least two different frogs[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.7955 mL 13.9774 mL 27.9548 mL 69.8871 mL
5 mM 0.5591 mL 2.7955 mL 5.5910 mL 13.9774 mL
10 mM 0.2795 mL 1.3977 mL 2.7955 mL 6.9887 mL
DMSO 15 mM 0.1864 mL 0.9318 mL 1.8637 mL 4.6591 mL
20 mM 0.1398 mL 0.6989 mL 1.3977 mL 3.4944 mL
25 mM 0.1118 mL 0.5591 mL 1.1182 mL 2.7955 mL
30 mM 0.0932 mL 0.4659 mL 0.9318 mL 2.3296 mL
40 mM 0.0699 mL 0.3494 mL 0.6989 mL 1.7472 mL
50 mM 0.0559 mL 0.2795 mL 0.5591 mL 1.3977 mL
60 mM 0.0466 mL 0.2330 mL 0.4659 mL 1.1648 mL
80 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8736 mL
100 mM 0.0280 mL 0.1398 mL 0.2795 mL 0.6989 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Desformylflustrabromine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Desformylflustrabromine951322-11-5DeformylflustrabrominedFBrnAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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