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RS 42358-197

Catalog No. T20739Cas No. 135729-55-4
Alias RS42358-197, RS-42358-197, RS 25259-007

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

RS 42358-197

RS 42358-197

Purity: 98.23%
Catalog No. T20739Alias RS42358-197, RS-42358-197, RS 25259-007Cas No. 135729-55-4
RS 42358-197 (RS 25259-007) is a competitive 5-HT3 receptor antagonist.
Pack SizePriceAvailabilityQuantity
1 mg$169In Stock
5 mg$391In Stock
10 mg$586In Stock
25 mg$870In Stock
50 mg$1,170In Stock
100 mg$1,570In Stock
200 mg$2,120In Stock
1 mL x 10 mM (in DMSO)$388In Stock
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Purity:98.23%
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Product Introduction

Bioactivity
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].
AliasRS42358-197, RS-42358-197, RS 25259-007
Chemical Properties
Molecular Weight330.85
FormulaC19H23ClN2O
Cas No.135729-55-4
Storage & Solubility Information
Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 11 mg/mL (33.25 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0225 mL15.1126 mL30.2252 mL151.1259 mL
5 mM0.6045 mL3.0225 mL6.0450 mL30.2252 mL
10 mM0.3023 mL1.5113 mL3.0225 mL15.1126 mL
20 mM0.1511 mL0.7556 mL1.5113 mL7.5563 mL

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