Silodosin-d4

Modify Date: 2024-01-13 15:08:45

Silodosin-d4 Structure
Silodosin-d4 structure
Common Name Silodosin-d4
CAS Number 1426173-86-5 Molecular Weight 499.559
Density 1.2±0.1 g/cm3 Boiling Point 601.4±55.0 °C at 760 mmHg
Molecular Formula C25H28D4F3N3O4 Melting Point N/A
MSDS N/A Flash Point 317.5±31.5 °C

 Use of Silodosin-d4


Silodosin-d4 (KAD 3213-d4) is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].

 Names

Name Silodosin-d4
Synonym More Synonyms

 Silodosin-d4 Biological Activity

Description Silodosin-d4 (KAD 3213-d4) is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Maxime Rossi , Silodosin in the treatment of benign prostatic hyperplasia. Drug Des Devel Ther. 2010; 4: 291–297.

[3]. Villa L, et al. Effects by silodosin on the partially obstructed rat ureter in vivo and on human and rat isolated ureters.Br J Pharmacol. 2013 May;169(1):230-8.

[4]. Osman NI, et al.Silodosin : a new subtype selective alpha-1 antagonist for the treatment of lower urinary tract symptoms in patients with benign prostatic hyperplasia.Expert Opin Pharmacother. 2012 Oct;13(14):2085-96.

[5]. Kawahara T, et al. Silodosin inhibits the growth of bladder cancer cells and enhances the cytotoxic activity of cisplatin via ELK1 inactivation.Am J Cancer Res. 2015 Sep 15;5(10):2959-68. eCollection 2015.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 601.4±55.0 °C at 760 mmHg
Molecular Formula C25H28D4F3N3O4
Molecular Weight 499.559
Flash Point 317.5±31.5 °C
Exact Mass 499.259613
LogP 2.52
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.552

 Synonyms

SILODOSIN-D4
1H-Indole-7-carboxamide, 2,3-dihydro-1-(3-hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl-1,1,2,2-d4]amino]propyl]-
1-(3-Hydroxypropyl)-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy](2H4)ethyl}amino)propyl]-7-indolinecarboxamide