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

Desformylflustrabromine hydrochloride (Synonyms: Deformylflustrabromine hydrochloride; dFBr hydrochloride)

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

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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10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
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50 mg USD 460 In-stock
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100 mg USD 810 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 105 mg/mL (293.53 mM)

*"≥" 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
10 mM 0.2795 mL 1.3977 mL 2.7955 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

357.72

Formula

C₁₆H₂₂BrClN₂

CAS No.

951322-11-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.77%

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Product Name:
Desformylflustrabromine hydrochloride
Cat. No.:
HY-107675
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Desformylflustrabromine hydrochloride

Cat. No.: HY-107675