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RS 42358-197 (RS 25259-007) is a competitive 5-HT3 receptor antagonist.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $169 | In Stock | In Stock | |
| 5 mg | $391 | In Stock | In Stock | |
| 10 mg | $586 | In Stock | In Stock | |
| 25 mg | $870 | In Stock | In Stock | |
| 50 mg | $1,170 | In Stock | In Stock | |
| 100 mg | $1,570 | - | In Stock | |
| 200 mg | $2,120 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $388 | In Stock | In Stock |
| Description | RS 42358-197 (RS 25259-007) is a competitive 5-HT3 receptor antagonist. |
| In vitro | RS 42358-197 acts against 5-HT-induced contractions in the guinea pig ileum (low-potency phase), yielding a pA2 estimate of 8.1[1]. |
| In vivo | In anesthetized rats. RS 42358-197, administered by the intravenous, intraduodenal or transdermal route, dose-dependently inhibited the Bezold-Jarisch reflex induced by 2-methyl 5-HT (ID50:0.05 micrograms/kg; i.v., 5.7 micrograms/kg; i.d., and 11.6 micrograms/chamber, respectively). In this regard, when administered intraduodenally, RS 42358-197 was more potent and exhibited a longer duration of action than either ondansetron or granisetron. In dogs, RS 42358-197, administered either intravenously or orally, dose-dependently inhibited the emesis induced by cisplatin, actinomycin and cyclophosphamide, but not that induced by apomorphine. When tested at maximally effective doses against cisplatin-induced emesis in dogs, RS 42358-197 had a longer duration of antiemetic activity (> 6 h) than ondansetron (2 h). RS 42358-197, administered orally, also afforded protection against cisplatin-induced emesis in ferrets. At doses that showed marked anti-emetic activity in dogs (10-100 micrograms/kg; i.v. and 100-1000 micrograms/kg; i.d.), RS 42358-197 did not produce any hemodynamic changes[1]. |
| Synonyms | RS42358-197, RS-42358-197, RS 25259-007 |
| Molecular Weight | 330.85 |
| Formula | C19H23ClN2O |
| Cas No. | 135729-55-4 |
| Smiles | O=C1C2=C3C(=CN1[C@H]4C5CCN(C4)CC5)CCCC3=CC=C2.Cl |
| Relative Density. | no data available |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 11 mg/mL (33.25 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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