80223-99-0
Chemical Structure
Tamsolusin hydrochloride
Synonym(s): YM12617 hydrochloride; LY253351 hydrochloride
- CAS No.: 80223-99-0
- Formula:C20H29ClN2O5S
- Molecular Weight:444.97
IUPAC Name: 5-(2-((2-(2-ethoxyphenoxy)ethyl)amino)propyl)-2-methoxybenzenesulfonamide hydrochloride
InChIKey: ZZIZZTHXZRDOFM-UHFFFAOYSA-N
SMILES: O=S(N)(C1=CC(CC(C)NCCOC2=C(OCC)C=CC=C2)=CC=C1OC)=O.Cl
Biological Activity: Tamsolusin hydrochloride (YM12617 hydrochloride; LY253351 hydrochloride) is an isomer of Tamsulosin (HY-B0661). Tamsolusin hydrochloride is a sulfonamide phenethylamine derivative and a competitive antagonist of selective post-synaptic α1-adrenoceptors. Tamsolusin hydrochloride inhibits CYP3A4 activity in a non-competitive, enantiomer-specific manner, with an IC50 and Ki of 6.75 μM. Tamsolusin hydrochloride produces dose-dependent hypotension, preferentially antagonizing α1-adrenoceptor-mediated pressor responses, and inhibits α2-adrenoceptor-mediated pressor responses at high doses. Tamsolusin hydrochloride can be used in research related to various diseases such as metabolism[1][2][3].
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Tamsolusin hydrochloride | Tamsolusin hydrochloride (YM12617 hydrochloride; LY253351 hydrochloride) is an isomer of Tamsulosin (HY-B0661). Tamsolusin hydrochloride is a sulfonamide phenethylamine derivative and a competitive antagonist of selective post-synaptic α1-adrenoceptors. Tamsolusin hydrochloride inhibits CYP3A4 activity in a non-competitive, enantiomer-specific manner, with an IC50 and Ki of 6.75 μM. Tamsolusin hydrochloride produces dose-dependent hypotension, preferentially antagonizing α1-adrenoceptor-mediated pressor responses, and inhibits α2-adrenoceptor-mediated pressor responses at high doses. Tamsolusin hydrochloride can be used in research related to various diseases such as metabolism. | |||||||||||||||||||||
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(Rac)-Tamsulosin-d3 hydrochloride | (Rac)-Tamsulosin-d3 hydrochloride is the deuterated-labeled Tamsolusin hydrochloride (HY-B0661C). Tamsolusin hydrochloride (YM12617 hydrochloride; LY253351 hydrochloride) is an isomer of Tamsulosin (HY-B0661). Tamsolusin hydrochloride is a sulfonamide phenethylamine derivative and a competitive antagonist of selective post-synaptic α1-adrenoceptors. Tamsolusin hydrochloride inhibits CYP3A4 activity in a non-competitive, enantiomer-specific manner, with an IC50 and Ki of 6.75 μM. Tamsolusin hydrochloride produces dose-dependent hypotension, preferentially antagonizing α1-adrenoceptor-mediated pressor responses, and inhibits α2-adrenoceptor-mediated pressor responses at high doses. Tamsolusin hydrochloride can be used in research related to various diseases such as metabolism. | |||||||||||||||||||||
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- [1]. Novotna A, et al. Profiling of enantiopure drugs towards aryl hydrocarbon (AhR), glucocorticoid (GR) and pregnane X (PXR) receptors in human reporter cell lines. Chemico-biological interactions. 2014 Feb 05;208:64-76. [Content Brief]
- [2]. Krasulova K, et al. Enantiospecific effects of chiral drugs on cytochrome P450 inhibition in vitro. Xenobiotica; the fate of foreign compounds in biological systems. 2016;46(4):315-24. [Content Brief]
- [3]. Honda K, et al. Further studies on (+/-)-YM-12617, a potent and selective alpha 1-adrenoceptor antagonist and its individual optical enantiomers. Naunyn-Schmiedeberg's archives of pharmacology. 1987 Sep;336(3):295-302. [Content Brief]
