1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Azasetron hydrochloride

Azasetron hydrochloride (Synonyms: Y-25130 hydrochloride)

Cat. No.: HY-B0068 Purity: >98.0%
Handling Instructions

Azasetron (hydrochloride) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

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

Azasetron hydrochloride Chemical Structure

Azasetron hydrochloride Chemical Structure

CAS No. : 123040-16-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in Water USD 117 In-stock
Estimated Time of Arrival: December 31
10 mg USD 106 In-stock
Estimated Time of Arrival: December 31
50 mg USD 384 In-stock
Estimated Time of Arrival: December 31
100 mg USD 720 In-stock
Estimated Time of Arrival: December 31
200 mg USD 960 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Azasetron (hydrochloride) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. Target: 5-HT3 Receptor Azasetron (hydrochloride) is a 5-HT3 receptor antagonist which is used as an anti-emetic. Azasetron (hydrochloride) inhibited the specific binding of [3H]quipazine to 5-HT3 receptors at the synaptic membranes of the rat cerebral cortex with a Ki value of 2.9 nM. Azasetron (hydrochloride) showed low affinity for histamine H1 receptors (IC50 = 4.4 microM) but it could not reveal any affinities for the other receptors (5-HT1A, 5-HT2, dopamine D1, dopamine D2, alpha 1-adrenoceptor, alpha 2-adrenoceptor, muscarine and benzodiazepine) even at a 10 microM concentration [1]. Azasetron (hydrochloride) (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. Azasetron (hydrochloride) is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone [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: 

H2O : ≥ 3.9 mg/mL (10.10 mM)

*"≥" means soluble, but saturation unknown.

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Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5889 mL 12.9443 mL 25.8886 mL
5 mM 0.5178 mL 2.5889 mL 5.1777 mL
10 mM 0.2589 mL 1.2944 mL 2.5889 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

386.27

Formula

C₁₇H₂₁Cl₂N₃O₃

CAS No.

123040-16-4

SMILES

O=C(C1=C(OCC(N2C)=O)C2=CC(Cl)=C1)NC3CN4CCC3CC4.[H]Cl

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Room temperature in continental US; may vary elsewhere

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Product Name:
Azasetron hydrochloride
Cat. No.:
HY-B0068
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Azasetron hydrochloride

Cat. No.: HY-B0068