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Azasetron dihydrochloride

Cat. No. M3201
Azasetron dihydrochloride Structure
Synonym:

Y-25130 2HCl; SENS-401 dihydrochloride

Size Price Availability Quantity
10mg USD 65  USD65 In stock
50mg USD 225  USD225 In stock
100mg USD 385  USD385 In stock
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Quality Control & Documentation
Biological Activity

Azasetron dihydrochloride is the hydrochloride form of Azasetron and is also an orally active 5-HT3 receptor antagonist for studies related to ear disorders such as sudden hearing loss.

Chemical Information
Molecular Weight 386.27
Formula C17H20ClN3O3.HCl
CAS Number 123040-16-4
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bao-Xia Fang, et al. Stability of azasetron-dexamethasone mixture for chemotherapy-induced nausea and vomiting administration

[2] Guanyang Lin, et al. Determination of azasetron hydrochloride in rabbit plasma by liquid chromatography tandem mass spectrometry and its application

[3] Yasuhiko Yamada, et al. Analysis of antiemetic effect of various dosage regimens of azasetron hydrochloride based on 5-HT3 receptor occupancy of serotonin

[4] Toru Hayakawa, et al. Comparison of ramosetron and azasetron for prevention of acute and delayed cisplatin-induced emesis in lung cancer patients

[5] K Katayama, et al. High affinity binding of azasetron hydrochloride to 5-hydroxytryptamine3 receptors in the small intestine of rats

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Keywords: Azasetron dihydrochloride, Y-25130 2HCl; SENS-401 dihydrochloride supplier, 5-HT Receptor, inhibitors, activators


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