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RS 17053 hydrochloride

RS 17053 hydrochloride
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.
Catalog No. T16798Cas No. 169505-93-5
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Purity:99.27%
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RS 17053 hydrochloride

Purity: 99.27%
Catalog No. T16798Alias RS-17053Cas No. 169505-93-5

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.
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Pack SizePriceAvailabilityQuantity
2 mg$34In Stock
5 mg$55In Stock
50 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$65In Stock
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Product Introduction

Bioactivity
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:9.8(PA2), α1A:(pki)9.1
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].
AliasRS-17053
Chemical Properties
Molecular Weight449.41
FormulaC24H30Cl2N2O2
Cas No.169505-93-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (278.14 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2251 mL11.1257 mL22.2514 mL111.2570 mL
5 mM0.4450 mL2.2251 mL4.4503 mL22.2514 mL
10 mM0.2225 mL1.1126 mL2.2251 mL11.1257 mL
20 mM0.1113 mL0.5563 mL1.1126 mL5.5628 mL
50 mM0.0445 mL0.2225 mL0.4450 mL2.2251 mL
100 mM0.0223 mL0.1113 mL0.2225 mL1.1126 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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