Name: Diazepam alkyne
Brand: AAT Bioquest
SKU: 50663
Price: 989 USD
Availability: InStock

Diazepam alkyne

Diazepam alkyne is a click chemistry-enabled benzodiazepine derivative that retains GABAA receptor binding while allowing bioorthogonal conjugation via copper-catalyzed azide-alkyne cycloaddition for developing receptor-targeted probes.

Bioorthogonal Reactivity: Contains a terminal alkyne group compatible with copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) for selective conjugation to azide-functionalized molecules
Pharmacophore Retention: Maintains the benzodiazepine core structure and activity, enabling studies on GABAA receptor interactions & related pharmacology
Versatile Probe Development: Ideal for synthesizing fluorescent, affinity, or photoactivatable probes for use in chemical biology & neuropharmacology
Live-Cell Compatibility: Suitable for intracellular labeling and target engagement studies in live-cell or in vivo systems
Research Applications: Facilitates structure–activity relationship (SAR) studies, target identification, and imaging of benzodiazepine derivatives in complex biological environments

The chemical structure of Diazepam alkyne.

Datasheet

SDS

COA

Catalog	Size	Price	Quantity
50663	1 mg	Price

Overview

Diazepam alkyne is an alkyne-functionalized derivative of diazepam designed for bioorthogonal conjugation via copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), commonly referred to as “click chemistry.” Incorporation of a terminal alkyne group enables site-specific and chemoselective coupling to azide-bearing molecules, including fluorophores, biotin derivatives, and solid-phase supports. The compound preserves the core benzodiazepine scaffold and pharmacophore of diazepam, facilitating its use in neuropharmacological research applications such as GABAA receptor binding assays, photoaffinity labeling, and probe development. Diazepam alkyne is particularly useful for generating functionalized analogs suitable for imaging, pull-down experiments, and structure–activity relationship (SAR) studies. Its compatibility with live-cell labeling strategies allows researchers to investigate the distribution, uptake, and target engagement of diazepam-like compounds in physiologically relevant systems. This reagent provides a powerful platform for elucidating benzodiazepine mechanisms of action at the molecular level.

Calculators

Common stock solution preparation

Table 1. Volume of DMSO needed to reconstitute specific mass of Diazepam alkyne to given concentration. Note that volume is only for preparing stock solution. Refer to sample experimental protocol for appropriate experimental/physiological buffers.

	0.1 mg	0.5 mg	1 mg	5 mg	10 mg
1 mM	237.006 µL	1.185 mL	2.37 mL	11.85 mL	23.701 mL
5 mM	47.401 µL	237.006 µL	474.012 µL	2.37 mL	4.74 mL
10 mM	23.701 µL	118.503 µL	237.006 µL	1.185 mL	2.37 mL

Molarity calculator

Enter any two values (mass, volume, concentration) to calculate the third.

Mass (Calculate)		Molecular weight		Volume (Calculate)		Concentration (Calculate)		Moles
mg	÷	421.93 g/mol	=	mL	x	mM	=	mmol

References

View all 6 references: Citation Explorer

Synthesis, Molecular Docking and In Vivo Biological Evaluation of Iminostilbene Linked 1,2,3-Triazole Pharmacophores as Promising Anti- Anxiety and Anti-Inflammatory Agents.

Authors:

Ankali, Kariyappa N and Rangaswamy, Javarappa and Shalavadi, Mallappa and Naik, Nagaraja

Journal:

Medicinal chemistry (Shariqah (United Arab Emirates)) (2022): 260-272

GABAergic mechanisms involved in the prepulse inhibition of auditory evoked cortical responses in humans.

Authors:

Inui, Koji and Takeuchi, Nobuyuki and Sugiyama, Shunsuke and Motomura, Eishi and Nishihara, Makoto

Journal:

PloS one (2018): e0190481

Facile synthesis of new imidazo[1,2-a]pyridines carrying 1,2,3-triazoles via click chemistry and their antiepileptic studies.

Authors:

Ulloora, Shrikanth and Shabaraya, Ramakrishna and Adhikari, Airody Vasudeva

Journal:

Bioorganic & medicinal chemistry letters (2013): 3368-72

The effects of diazepam on sensory gating in healthy volunteers.

Authors:

van Luijtelaar, Gilles

Journal:

Neuroscience letters (2003): 65-8

Effects of (-)-baclofen, clonazepam, and diazepam on tone exposure-induced hyperexcitability of the inferior colliculus in the rat: possible therapeutic implications for pharmacological management of tinnitus and hyperacusis.

Authors:

Szczepaniak, W S and Møller, A R

Journal:

Hearing research (1996): 46-53

Physical properties

Molecular weight	421.93
Solvent	DMSO

Storage, safety and handling

H-phrase	H303, H313, H333
Hazard symbol	XN
Intended use	Research Use Only (RUO)
R-phrase	R20, R21, R22
Storage	Freeze (< -15 °C); Minimize light exposure

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Page updated on May 9, 2026