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RS 17053 hydrochloride is a potent and selective antagonist of the α1A adrenoceptor, with a pKi value of 9.1 in native cell membranes and a pA2 value of 9.8 in functional assays.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $34 | In Stock | |
| 5 mg | $55 | In Stock | |
| 50 mg | Preferential | In Stock | |
| 1 mL x 10 mM (in DMSO) | $65 | In Stock |
| Description | RS 17053 hydrochloride is a potent and selective antagonist of the α1A adrenoceptor, with a pKi value of 9.1 in native cell membranes and a pA2 value of 9.8 in functional assays. |
| Targets&IC50 | α1A-adrenoceptor:(pki)9.1 , α1A-adrenoceptor:9.8(PA2) |
| In vitro | RS 17053 hydrochloride antagonizes responses to NE only at high concentrations in isolated smooth muscle preparations from human LUT tissues. RS 17053 hydrochloride displays a high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8) in several tissues from rat and cloned adrenoceptors [1]. |
| In vivo | RS 17053 hydrochloride exhibits a rapid onset and a duration of action exceeding 60 minutes. At a dosage of 10 mg/kg, RS-17053 significantly suppresses food intake and its pretreatment notably alters food intake [F(4, 132) = 6.28, p < 0.0001] [2]. |
| Synonyms | RS-17053 |
| Molecular Weight | 449.41 |
| Formula | C24H30Cl2N2O2 |
| Cas No. | 169505-93-5 |
| Smiles | Cl.CC(C)(Cc1c[nH]c2ccc(Cl)cc12)NCCOc1ccccc1OCC1CC1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 125 mg/mL (278.14 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.9 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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