Lerisetron
CAS No. : 143257-98-1
| Size | Price | Stock |
|---|---|---|
| 5mg | $160 | In-stock |
| 10mg | $250 | In-stock |
| 25mg | $425 | In-stock |
| 50mg | $620 | In-stock |
| 100mg | $890 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-105090 |
| M.Wt: | 292.39 |
| Formula: | C18H20N4 |
| Purity: | >98 % |
| Solubility: | DMSO : 25 mg/mL (ultrasonic) |
Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats[1].
IC50 & Target: pKi: 9.2 (5-HT3)[1]
In Vivo: Lerisetron (50-200 μg/kg; IV; single) exhibits CL of 0.004-0.005 L/min, Vds of 0.88-0.96 L, MRT0-LAST of 224-337.1 min and AUC∞ of 57.7-66.1 μg·min/L in rats[2].
Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia[2].
Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats[2].
| IV (50 μg/kg) | IV (100 μg/kg) | IV (200 μg/kg) | |
| CL (L/min) | 0.005 | 0.004 | 0.004 |
| Vds (L) | 0.9 | 0.88 | 0.96 |
| MRT0-LAST (min) | 224 | 337.1 | 226.3 |
| AUC∞ (μg·min/L) | 66.1 | 57.7 | 58.1 |
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