| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
With an affinity (Ki) of 115 nM in rat cerebral cortex, 150 nM in NG 108-15 cell membranes, and 103 nM in the entire NG 108-15 cell, SR 57227A binds to 5-HT3 receptors tagged with [3H]S-zacopride[1].
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| ln Vivo |
In the forced swimming test, SR 57227A (1–30 mg/kg; ip) reduces immobility time in a dose-dependent manner; its ED50 value is 14.2 mg/kg[2]. SR 57227A dose-dependently shortens the rats' period of immobility following intraperitoneal injection in the forced swimming test. Following oral dosing, SR 57227A is also active in both species (ED50=7.6 mg/kg ip in rats). In a mouse time-course investigation, SR 57227A (20 mg/kg po) has a noteworthy 6-hour duration of effect. In the final two days of the avoidance task, SR 57227A (1 and 3 mg/kg ip) decreases the elevation of escape failures in the learned helplessness paradigm in rats by 50–60%. It also lessens isolation-induced aggressivity in mice by 50–85%, an effect that is countered by Zacopride (1 mg/kg ip)[2].
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| References |
[1]. Poncelet M, et al, Le Fur G. Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83‐90.
[2]. Bachy A, et al. SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo. Eur J Pharmacol. 1993;237(2-3):299‐309. |
| Molecular Formula |
C10H15CL2N3
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|---|---|
| Molecular Weight |
248.15
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| CAS # |
77145-61-0
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
Cl.NC1CCN(C2C=CC=C(Cl)N=2)CC1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 33.33 mg/mL (134.31 mM)
DMSO: 8.33 mg/mL (33.57 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (40.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0298 mL | 20.1491 mL | 40.2982 mL | |
| 5 mM | 0.8060 mL | 4.0298 mL | 8.0596 mL | |
| 10 mM | 0.4030 mL | 2.0149 mL | 4.0298 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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