Silodosin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效的尿选择性 α1a-肾上腺素受体拮抗剂，Ki 为 36 pM；对 α1b 和 α1d 尊重者的效力分别低 583 倍和 56 倍。

A highly potent, uroselective α1a-adrenoceptor antagonist with Ki of 36 pM; displays 583- and 56-fold lower potency against α1b and α1d respectors, respectively; inhibits norepinephrine-induced increases intracellular Ca2+ concentrations in CHO cells with IC50 of 0.32 nM; inhibits intraurethral pressure (IUP) response in vivo.Other Indication Approved(In Vitro):Silodosin (KAD 3213; KMD 3213) inhibits norepinephrine-induced increases in intracellular Ca2+ concentrations in alpha 1a-AR-expressing Chinese hamster ovary cells with an IC50 of 0.32 nM but had a much weaker inhibitory effect on the alpha 1b- and alpha 1d-ARs.Silodosin potently inhibits 2-[2-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl]-alpha-tetralone binding to the cloned human alpha 1a-AR, with a Ki value of 0.036 nM, but has 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively.Silodosin (0-10 μM; 24 hours) decreases ELK1 gene expression as a dose-dependent manner in all the bladder cancer cell lines.Silodosin (0-10 μM; 24 hours) decreases ELK1 protein expression as a as a dose-dependent manner.Silodosin (0-10 μM; 96 hours) insignificantly changes cell viability of AR-positive UMUC3 or TCCSUP cultured in an androgen-depleted condition or that of AR-negative 647V. In contrast, silodosin reduced the growth of UMUC3 cells cultured with normal FBS containing androgens (58% decrease at 10 μM).(In Vivo):Silodosin (intravenous injection; 0.1-0.3mg/kg) reduces the obstruction-induced increases in MinP by 27.7 % (0.1 mg/kg) and 20.8 %(0.3 mg/kg). It improves detrusor overactivity and reduces the grade of obstruction, and thus may be effective for both storage and voiding dysfunction for the treatment of LUTS/BPH.

Silodosin (KAD 3213; KMD 3213) inhibits norepinephrine-induced increases in intracellular Ca2+ concentrations in alpha 1a-AR-expressing Chinese hamster ovary cells with an IC50 of 0.32 nM but had a much weaker inhibitory effect on the alpha 1b- and alpha 1d-ARs.Silodosin potently inhibits 2-[2-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl]-alpha-tetralone binding to the cloned human alpha 1a-AR, with a Ki value of 0.036 nM, but has 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively.Silodosin (0-10 μM; 24 hours) decreases?ELK1 gene expression as a dose-dependent manner in all the bladder cancer cell lines. Silodosin (0-10 μM; 24 hours) decreases ELK1 protein expression as a as a dose-dependent manner.Silodosin (0-10 μM; 96 hours) insignificantly changes cell viability of AR-positive UMUC3or TCCSUP cultured in an androgen-depleted condition or that of AR-negative 647V.In contrast, silodosin reduced the growth of UMUC3 cells cultured with normal FBS containing androgens (58% decrease at 10 μM). RT-PCR Cell Line:TCCSUP; UMUC3 and 647V cells Concentration:0.1, 0.5, 3.0, or 10 μM Incubation Time:24 hours Result:Decreases ELK1 in bladder cancer cells.Western Blot Analysis Cell Line:TCCSUP; UMUC3 and 647V cells Concentration:0.1, 0.5, 3.0, or 10 μM Incubation Time:24 hours Result:Decreases ELK1 in bladder cancer cells.Cell Proliferation Assay Cell Line:UMUC3,TCCSUP or AR-negative 647V cells Concentration:0.1, 0.5, 3.0, or 10 μM Incubation Time:96 hours Result:Decreased cell viability of UMUC3 cells cultured with normal FBS containing androgens (58% decrease).

Silodosin (intravenous injection; 0.1-0.3mg/kg) reduces the obstruction-induced increases in MinP by 27.7 % (0.1 mg/kg) and 20.8 %(0.3 mg/kg). It improves detrusor overactivity and reduces the grade of obstruction, and thus may be effective for both storage and voiding dysfunction for the treatment of LUTS/BPH. Animal Model:Sprague Dawley ratsDosage:0.1-0.3mg/kg Administration:Intravenous injection Result:Effectively reduced contractions of both human and rat isolated ureters.

KAD 3213 | KMD 3213

GPCR/G Protein

Adrenergic Receptor

β-adrenergicreceptor

Other Indications

Other Disease

160970-54-7

495.5345

C25H32F3N3O4

>98% (HPLC)

10 mM in DMSO

O=C(C1=CC(C[C@H](NCCOC2=CC=CC=C2OCC(F)(F)F)C)=CC3=C1N(CCCO)CC3)N

1H-Indole-7-carboxamide, 2,3-dihydro-1-(3-hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-

(-20℃)

With Ice Pack

≥ 2 years