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Submit ReviewRS 17053 hydrochloride
说明： α1A antagonist
化学名： (N-[2-(2-Cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α,α-dimethyl-1H-indole-3-ethanamine) hydrochloride
生物活性 for RS 17053 hydrochloride
RS 17053 hydrochloride is an α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8).
许可信息
Sold with the permission of Roche Bioscience
技术数据 for RS 17053 hydrochloride
| 分子量 | 449.42 |
| 公式 | C24H29N2O2Cl.HCl |
| 储存 | Store at RT |
| CAS Number | 169505-93-5 |
| PubChem ID | 9824953 |
| InChI Key | QFOPFGRPNPCPBX-UHFFFAOYSA-N |
| Smiles | Cl.CC(C)(CC1=CNC2=CC=C(Cl)C=C12)NCCOC1=C(OCC2CC2)C=CC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for RS 17053 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 4.49 | 10 | |
| DMSO | 22.47 | 50 |
制备储备液 for RS 17053 hydrochloride
以下数据基于产品分子量 449.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.45 mL | 22.25 mL | 44.5 mL |
| 2.5 mM | 0.89 mL | 4.45 mL | 8.9 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.45 mL |
| 25 mM | 0.09 mL | 0.45 mL | 0.89 mL |
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产品说明书 for RS 17053 hydrochloride
参考文献 for RS 17053 hydrochloride
参考文献是支持产品生物活性的出版物。
Ford et al (1996) 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 huma Mol.Pharmacol. 49 209 PMID: 8632751
Marshall et al (1996) Different subtypes of α1A-adrenoceptor mediating contraction of rat epididymal vas deferens, rat hepatic portal vein and human prostate distinguished by the antagonist RS 17053. Br.J.Pharmacol. 119 407 PMID: 8886428
Ford et al (1995) Do α1A (α1C)-adrenoceptors (AR) mediate prostatic smooth muscle contraction in man? Studies with a novel, selective α1A-AR antagonist, RS 17053. Br.J.Pharmacol. 114 C25
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.