Sazetidine A dihydrochloride

Name: Sazetidine A dihydrochloride
Brand: Tocris Bioscience
SKU: 2736

Tocris Bioscience, part of Bio-Techne | Catalog # 2736

Citations (9)

COA / SDS

α4β2 nAChR ligand; may act as an agonist or a desensitizer

Key Product Details

Description:	α4β2 nAChR ligand; may act as an agonist or a desensitizer
Chemical Name:	6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	333.25

View Full Technical Details for Sazetidine A dihydrochloride

Technical Data
Citations

Biological Activity for Sazetidine A dihydrochloride

Sazetidine A dihydrochloride is a subtype-selective α4β2 nicotinic acetylcholine receptor ligand (K_i values are 0.26 and 54 nM at α4β2 and α3β4 receptors respectively). May act as a silent desensitizer or as an agonist, depending on subunit stoichiometry (EC₅₀ = 1.1 nM for nAChR-stimulated dopamine release). Exhibits analgesic activity in vivo and significantly reduces nicotine self-administration in an experimental rat model.

Technical Data for Sazetidine A dihydrochloride

M. Wt	333.25
Formula	C₁₅H₂₀N₂O₂.2HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2455450-63-0
PubChem ID	56972183
InChi Key	WRSKKJWUXISFFU-UTLKBRERSA-N
Smiles	OCCCCC#CC1=CN=CC(OC[C@H]2NCC2)=C1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Sazetidine A dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	16.66	50

Preparing Stock Solutions for Sazetidine A dihydrochloride

The following data is based on the product molecular weight 333.25.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	6.00 mL	30.01 mL	60.02 mL
2.5 mM	1.20 mL	6.00 mL	12.00 mL
5 mM	0.60 mL	3.00 mL	6.00 mL
25 mM	0.12 mL	0.60 mL	1.20 mL

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References for Sazetidine A dihydrochloride

References are publications that support the biological activity of the product.

Zwart Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors. Mol.Pharmacol.
Cucchiaro Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug. Anesthesiology 2008 PMID: 18719450
Levin Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats. J.Pharmacol.Exp.Ther. 2010 PMID: 20007754
Xiao Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them. Mol.Pharmacol. 2006 PMID: 16857741