An α1A-adrenergic receptor antagonist
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RS 17053 (hydrochloride)

Item No. 33548

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-chloro-N-[2-[2-(cyclopropylmethoxy)phenoxy]ethyl]-α,α-dimethyl-1H-indole-3-ethanamine, monohydrochloride
CAS Number
169505-93-5
Molecular Formula
C24H29ClN2O2 • HCl
Formula Weight
449.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mMEthanol: 10 mM
SMILES
CC(NCCOC1=C(OCC2CC2)C=CC=C1)(C)CC3=CNC4=C3C=C(Cl)C=C4.Cl
InChi Code
InChI=1S/C24H29ClN2O2.ClH/c1-24(2,14-18-15-26-21-10-9-19(25)13-20(18)21)27-11-12-28-22-5-3-4-6-23(22)29-16-17-7-8-17;/h3-6,9-10,13,15,17,26-27H,7-8,11-12,14,16H2,1-2H3;1H
InChi Key
QFOPFGRPNPCPBX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $193

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    25 mg

    $448

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    Product Description

    RS 17053 is an α1A-adrenergic receptor (α1A-AR) antagonist.1 It selectively binds to the α1A-AR (Ki = 2.5 nM) over α1B- and α1D-ARs (Kis = 50 and 79 nM, respectively). RS 17053 inhibits norepinephrine-induced contractions in isolated rat kidney and mesenteric arteries (pA2s = 9.8 and 9.9, respectively), tissues that endogenously express high levels of α1A-AR, and, to a lesser extent, in isolated rat aortic rings, which highly express α1D-ARs, and human lower urinary tract tissue (pA2s = 7.7 and 7.3, respectively).2 It also inhibits phenylephrine-induced increases in mean arterial pressure (MAP) in normotensive and spontaneously hypertensive rats (ED50s = 528 and 533 µg/kg, respectively).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kenny, B.A., Miller, A.M., Williamson, I.J.R., et al. Evaluation of the pharmacological selectivity profile of α1 adrenoceptor antagonists at prostatic α1 adrenoceptors: Binding, functional and in vivo studies. Br. J. Pharmacol. 118(4), 871-878 (1996).

    2. Ford, A.P.D.W., Arrendondo, N.F., Blue, D.R., Jr., et al. RS-17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α, α-dimethyl-1H-indole-3-ethanamine hydrochloride), a selective α1A-adrenoceptor antagonist, displays low affinity for functional α1-adrenoceptors in human prostate: Implications for adrenoceptor classification. Mol. Pharmacol. 49(2), 209-215 (1996).

    3. Qi, X., Weizhong, Z., Zhizhen, L., et al. α1A-adrenergic receptor mediated pressor response to phenylephrine in anesthetized rat. Sci. China C. Life Sci. 47(1), 59-65 (2004).