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Home / Biochemicals / Small Molecules

Azasetron hydrochloride

SKU : BHB21300379

A Potent Antagonist of Serotonin-Gated Channels

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Mfr.No.	Y-100, Y-100_10 mg, Y-100_25 mg, Y-100_5 mg, Y-100_50 mg
Description	Azasetron hydrochloride (#Y-100) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C17H21Cl2N3O3.
Synonyms	Synthetic
Background	Azasetron hydrochloride (Y-25130 hydrochloride) is a potent 5-HT3 receptor antagonist. It selectively and competitively binds 5-HT3 receptors thereby blocking the serotonin binding site. Azasetron is classified as a derivative of benzamide. It has a different chemical structure from other 5-HT3 receptor blockers. The significant difference is found in the pharmacokinetic profiles resulting in a longer duration of action and a higher affinity for the 5-HT3 receptor1,2. Azasetron has an IC50 value ~4.9x10-10 M4 and half life of 5.4 hours3.The 5-HT3 receptor subtype is a member of the Cys-loop ligand-gated cation channels which are expressed throughout the central and peripheral nervous systems and mediate a variety of physiological functions5.Azasetron is mostly administered orally and by I.V (60-70%) and excreted in the urine in an unmetabolized form. Orally-administered azasetron is shown to be absorbed and secreted by the saturable transport mechanism in the small intestine, resulting in good bioavailability (approximately 90%)2.5-HT3 receptor antagonists have been established in a number of clinical trials as effective agents in the management and prevention of nausea and vomiting caused by cancer chemotherapy as well as postoperative nausea and emesis after anesthesia and surgery1,3.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	0.1-100 nM.
Reconstitution	100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
Cas Number	123040-16-4
Molecular Weight	386.3
Solubility	100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
Target	5-HT3 receptors
Activity	Azasetron hydrochloride is a potent 5-HT3 channel blocker with a Ki ~2.9 nM1.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: N-(1-azabicyclo(2.2.2)octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide;hydrochloride.

Purity	>98%
Form	Lyophilized powder.
Storage	Storage of solutions: Up to four weeks at 4°C or three months at -20°C.

Product Manual	SDS

Reference	Lee. H.Y. et al. (2014) Cancer Res. Treat. 46, 19. Tsukagoshi, S. (1999) Gan To Kagaku Ryoho 26, 1001. Yun, M.J. et al. (2010) Yonsei Med. J. 51, 88. Yakushiji,T. and Akaike, N. (1992) Br. J. Pharmacol. 107, 853. Kato, S. et al. (2013) Biol. Pharm. Bull. 36,1406. Fukuda, T. et al. (1991) Eur. J. Pharmacol. 196, 299.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300379-1	Y-100_10 mg	10 mg	$117		Add to Cart
BHB21300379-2	Y-100_25 mg	25 mg	$263		Add to Cart
BHB21300379-3	Y-100_5 mg	5 mg	$85		Add to Cart
BHB21300379-4	Y-100_50 mg	50 mg	$476		Add to Cart

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