Silodosin

Modify Date: 2024-01-02 12:25:56

Silodosin structure	Common Name	Silodosin
	CAS Number	160970-54-7	Molecular Weight	495.534
	Density	1.2±0.1 g/cm3	Boiling Point	601.4±55.0 °C at 760 mmHg
	Molecular Formula	C₂₅H₃₂F₃N₃O₄	Melting Point	107 °C
	MSDS	N/A	Flash Point	317.5±31.5 °C

Use of Silodosin

Silodosin (Rapaflo; KMD-3213) is an α1-adrenoceptor antagonist with high uroselectivity; In treatment of dysuria.IC50 Value:Target: Adrenergic Receptorin vitro: Silodosin potently inhibited 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 had 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively. Silodosin inhibited 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.in vivo: Using pharmacologically well characterized native rat tissues [submaxillary gland (alpha 1A-AR-expressing tissue), liver (alpha 1B-AR-expressing tissue), and heart (mixed alpha 1A- and alpha 1B-AR-expressing tissue)], binding studies showed that inhibition curves for Silodosin in submaxillary gland and liver best fit a one-site model (with Ki values of 0.15 and 16 nM, respectively), whereas Silodosin had high and low affinity sites in heart membranes. Chloroethylclonidine treatment of rat heart membranes completely eliminated the low affinity sites for Silodosin. Furthermore, in human liver and prostate Silodosin could identify high and low affinity sites, the Ki values of which corresponded well to those for the cloned human alpha 1a- and alpha 1b-ARs, respectively. Moreover, the affinity of Silodosin was found to be approximately 10-fold higher at the cloned human alpha 1a-AR than at the cloned rat alpha 1a-AR.v

Name	1-(3-hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethylamino]propyl]-2,3-dihydroindole-7-carboxamide
Synonym	More Synonyms

Description	Silodosin (Rapaflo; KMD-3213) is an α1-adrenoceptor antagonist with high uroselectivity; In treatment of dysuria.IC50 Value:Target: Adrenergic Receptorin vitro: Silodosin potently inhibited 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 had 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively. Silodosin inhibited 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.in vivo: Using pharmacologically well characterized native rat tissues [submaxillary gland (alpha 1A-AR-expressing tissue), liver (alpha 1B-AR-expressing tissue), and heart (mixed alpha 1A- and alpha 1B-AR-expressing tissue)], binding studies showed that inhibition curves for Silodosin in submaxillary gland and liver best fit a one-site model (with Ki values of 0.15 and 16 nM, respectively), whereas Silodosin had high and low affinity sites in heart membranes. Chloroethylclonidine treatment of rat heart membranes completely eliminated the low affinity sites for Silodosin. Furthermore, in human liver and prostate Silodosin could identify high and low affinity sites, the Ki values of which corresponded well to those for the cloned human alpha 1a- and alpha 1b-ARs, respectively. Moreover, the affinity of Silodosin was found to be approximately 10-fold higher at the cloned human alpha 1a-AR than at the cloned rat alpha 1a-AR.v
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Endocrinology
References	[1]. Kobayashi, Shinya; Tomiyama, Yoshitaka; Effects of silodosin and tamsulosin on the urethra and cardiovascular system in young and old dogs with benign prostatic hyperplasia. European Journal of Pharmacology (2009), 613(1-3), 135-140. [2]. Tatemichi, Satoshi; Tomiyama, Yoshitaka; Maruyama, Itaru; Uroselectivity in male dogs of silodosin (KMD-3213), a novel drug for the obstructive component of benign prostatic hyperplasia. Neurourology and Urodynamics (2006), 25(7), 792-794. [3]. Osman NI, Chapple CR, Cruz F, Desgrandchamps F, Llorente C, Montorsi F.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 Oc [4]. Cui Y, Zong H, Zhang Y.The efficacy and safety of silodosin in treating BPH: a systematic review and meta-analysis.Int Urol Nephrol. 2012 Aug 24. [5]. Goseki T, Ishikawa H, Ogasawara S, Mashimo K, Nemoto N, Taguchi Y, Yago K, Shimizu K.Effects of tamsulosin and silodosin on isolated albino and pigmented rabbit iris dilators: Possible mechanism of intraoperative floppy-iris syndrome.J Cataract Refract Su

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Endocrinology

References

[1]. Kobayashi, Shinya; Tomiyama, Yoshitaka; Effects of silodosin and tamsulosin on the urethra and cardiovascular system in young and old dogs with benign prostatic hyperplasia. European Journal of Pharmacology (2009), 613(1-3), 135-140.

[2]. Tatemichi, Satoshi; Tomiyama, Yoshitaka; Maruyama, Itaru; Uroselectivity in male dogs of silodosin (KMD-3213), a novel drug for the obstructive component of benign prostatic hyperplasia. Neurourology and Urodynamics (2006), 25(7), 792-794.

[3]. Osman NI, Chapple CR, Cruz F, Desgrandchamps F, Llorente C, Montorsi F.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 Oc

[4]. Cui Y, Zong H, Zhang Y.The efficacy and safety of silodosin in treating BPH: a systematic review and meta-analysis.Int Urol Nephrol. 2012 Aug 24.

[5]. Goseki T, Ishikawa H, Ogasawara S, Mashimo K, Nemoto N, Taguchi Y, Yago K, Shimizu K.Effects of tamsulosin and silodosin on isolated albino and pigmented rabbit iris dilators: Possible mechanism of intraoperative floppy-iris syndrome.J Cataract Refract Su

Density	1.2±0.1 g/cm3
Boiling Point	601.4±55.0 °C at 760 mmHg
Melting Point	107 °C
Molecular Formula	C₂₅H₃₂F₃N₃O₄
Molecular Weight	495.534
Flash Point	317.5±31.5 °C
Exact Mass	495.234497
PSA	97.05000
LogP	2.52
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.552

Hazard Codes	Xi

1-(3-Hydroxypropyl)-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]-7-indolinecarboxamide

KAD 3213

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

[3H]-Silodosin

Rapaflo

[14C]-Silodosin

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

UNII-CUZ39LUY82

Silodyx

Urief

Silodosin

KMD-3213

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Silodosin
Price: Click To Check
Purity: 99.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Silodosin
Price: ￥1968.0/100mg ￥568.0/5mg ￥1058.0/25mg
Purity: 99.0%
Delivery: 2 Day
Contact: Liu jia
Email: 2130147988@qq.com

DC Chemicals Limited
China
Product Name: Silodosin
Price: $350.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: Silodosin
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

Henan Tianfu Chemical Co., Ltd.
China
Product Name: Silodosin
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Delivery: Inquiry
Contact: Anson
Email: info@tianfuchem.com

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