General
Preferred name
SILODOSIN
Synonyms
KAD 3213 ()
KMD 3213 ()
KAD 3213, KMD 3213 ()
KAD-3213 ()
URIEF ()
UROREC ()
RAPAFLO ()
RAPILIF ()
SILODOSINE ()
Silodosin recordati ()
KSO-0400 ()
SILODYX ()
KMD-3213 ()
SILODOSINA ()
SILODAL ()
Silodosin-d4 ()
SILODOSIN RECORDATI ()
P&D ID
PD009321
CAS
160970-54-7
1426173-86-5
Tags
available
drug
Approved by
EMA
FDA
First approval
2008
Drug indication
Benign prostatic hyperplasia
Drug Status
approved
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
ABSORPTION Quickly absorbed and has a bioavailability of 32% at 8mg/day (therapeutic dose).; When 8 mg of silodosin is taken once daily with food, the pharmacokinetic parameters are as follows: ; Cmax = 61.6 ± 27.54 ng/mL;; Tmax = 2.6 ± 0.90 hours; ; AUC (0h-24h) = 373 ng•hr/ml. ; The AUC of its metabolite, KMD3213G, is four times greater than silodosin.
ROE Fecal (54.9%); ; Renal (33.5%)
HALF-LIFE Silodosin = 13.3 ± 8.07 hours;; KMD-3213G = 24 hours;
DESCRIPTION Silodosin an α1-adrenoceptor antagonist with selectivity for prostate adrenoceptors (mainly the α1A subtype). (GtoPdb)
MOA Benign prostate hyperplasia (BPH), or an enlarged prostate, is a condition found only in men and is characterized by a non-cancerous enlargement of the prostate gland. Symptoms of BPH include urinary difficulty, urinary frequency and an inability to complete bladder emptying. Silodosin is highly uroselective for the alpha (1A) receptors located in the prostate, [urethrea and bladder trigone in the lower urinary tract]. Blocking these receptors relaxes the smooth muscles, resulting in an improvement in urine flow and a reduction in BPH symptoms. The selective binding of silodosin to the alpha (1A) receptors is substantially greater than the binding to the cardiovascular-associated alpha (1B) receptors and thereby maximizes target organ activity while minimizing the potential for blood pressure effects. [Watson Pharmaceutical Inc. Press release] Silodosin is alpha 1A-adrenoceptor selective antagonist which inhibits sympathetic nerve stimulation and relaxation of smooth muscle tone in the lower urinary tract which relieves the pressure from contraction of smooth muscle. The reduction of intraurethral pressure improves voiding and storage issues associated with BPH. ; ; ; ;
DESCRIPTION Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active ¦Á1A-adrenergic receptor (¦Á1A-AR) blocker. Silodosin exhibits high affinity for ¦Á1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for ¦Á1B-AR and ¦Á1D-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].
PRICE 51
DESCRIPTION Selective GPR55 agonist; also promotes NSC proliferation and differentiation (Tocris Bioactive Compound Library)
DESCRIPTION Silodosin is an alpha-1 adrenergic receptor antagonist used to treat symptoms associated with benign prostatic hyperplasia (BPH). (Enamine Bioactive Compounds)
DESCRIPTION Silodosin (KAD 3213) is an alpha-Adrenergic Blocker. The mechanism of action of silodosin is as an Adrenergic alpha-Antagonist. (TargetMol Bioactive Compound Library)
Compound Sets
29
Axon Medchem Screening Library
3112
Cayman Chemical Bioactives
14866
30236
ChEMBL Approved Drugs
CHEMBL24778
ChEMBL Drugs
CHEMBL24778
Concise Guide to Pharmacology 2017/18
493
Concise Guide to Pharmacology 2019/20
493
Concise Guide to Pharmacology 2021/22
493
Concise Guide to Pharmacology 2023/24
493
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB06207
DrugBank Approved Drugs
DB06207
DrugCentral
4151
DrugCentral Approved Drugs
4151
DrugMAP
DMJSBT6
DrugMAP Approved Drugs
DMJSBT6
Enamine Bioactive Compounds
EBC-27231
EU-OPENSCREEN Bioactive Compound Library
EOS101411
EUbOPEN Chemogenomics Library
EUB0000381
Guide to Pharmacology
493
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL24778
MedChem Express Bioactive Compound Library
HY-10122
NCATS Inxight Approved Drugs
CUZ39LUY82
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
Silodosin(Rapaflo)
TargetMol Bioactive Compound Library
T1504
Tocris Bioactive Compound Library
6663
VGSC-DB
NA0188
External IDs
38
Properties
(calculated by RDKit )
Molecular Weight
495.23
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
3
Rotatable Bonds
13
Ring Count
3
Aromatic Ring Count
2
cLogP
3.07
TPSA
97.05
Fraction CSP3
0.48
Chiral centers
1.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Adrenergic Receptor
β-adrenergic receptor
ADRA1A, ADRA1B, ADRA1D
a1A antagonist
Bacterial
Primary Target
Adrenergic ?1 Receptors
MOA
Antagonist
Adrenergic Receptor antagonist
Indication
benign prostatic hyperplasia (BPH)
Pathway
GPCR/G protein
Neuroscience
Anti-infection
Neuronal Signaling
VGSC Target
Nav1.5
Recommended Cell Concentration
100 nM
Source data