RS 17053 hydrochloride (RS-17053)

  Cat. No.:  DC12250  
Chemical Structure
169505-93-5
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Field of application
RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
Cas No.: 169505-93-5
SMILES: [H]Cl.ClC1=CC2=C(NC=C2CC(C)(C)NCCOC3=CC=CC=C3OCC4CC4)C=C1
Formula: C24H30Cl2N2O2
M.Wt: 449.41
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: In Vitro In several tissues from rat and cloned adrenoceptors, RS 17053 hydrochloride displays 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). However, in isolated smooth muscle preparations from human LUT tissues, RS 17053 hydrochloride antagonizes responses to NE only at high concentrations. Estimates of affinity (pA2) at α1-adrenoceptors mediating NE-induced contractions are 7.5 in prostatic periurethral longitudinal smooth muscle (compared with 8.6 for prazosin), 6.9 in anterior fibromuscular stroma (prazosin, 8.9), and 7.1 in bladder neck (prazosin, 8.5). In Vivo RS 17053 hydrochloride has a rapid onset of action, and a duration of action exceeding 60 min. RS 17053 hydrochloride pretreatment significantly alteres food intake [F(4, 132) 5 6.28, p , 0.0001]. 10 mg/kg RS-17053 significantly suppresses food intake.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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