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      Silodosin (KAD 3213; KMD 3213)
      Silodosin (KAD 3213; KMD 3213)

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      This product is for research use only, not for human use. We do not sell to patients.
      Number： - + Pieces（InventoryPieces）
      InvivoChem Cat #: V1111
      CAS #: 160970-54-7Purity ≥98%

      Description: Silodosin (KMD-3213; KMD3213;  KAD3213; KAD-3213; Silodosin; trade names Rapaflo, Silodal, Silodyx, Rapilif, Urief, Urorec) is a highly selective alpha1A/α1A-adrenoceptor antagonist that was approved for the treatment of BPH-benign prostatic hyperplasia.  

      References: Yakugaku Zasshi. 2006 Mar;126 Spec no.:209-16; Yakugaku Zasshi. 2006 Mar;126 Spec no.:231-6.

      Related CAS: 879292-24-7 (Silodosin glucuronide sodium)

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      Molecular Weight (MW)495.53 
      FormulaC25H32F3N3O4 
      CAS No.160970-54-7 
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 99 mg/mL (199.8 mM)  
      Water: <1 mg/mL
      Ethanol: 99 mg/mL (199.8 mM)  
      Other info

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

      InChi Key: PNCPYILNMDWPEY-QGZVFWFLSA-N

      InChi Code: InChI=1S/C25H32F3N3O4/c1-17(30-8-12-34-21-5-2-3-6-22(21)35-16-25(26,27)28)13-18-14-19-7-10-31(9-4-11-32)23(19)20(15-18)24(29)33/h2-3,5-6,14-15,17,30,32H,4,7-13,16H2,1H3,(H2,29,33)/t17-/m1/s1

      SMILES Code: O=C(C1=CC(C[[email protected]](NCCOC2=CC=CC=C2OCC(F)(F)F)C)=CC3=C1N(CCCO)CC3)N

      SynonymsKAD 3213, KMD 3213; KMD 3213; KAD 3213; KMD-3213; KMD3213;  KAD 3213; KAD3213; Silodosin. trade names Rapaflo, Silodyx, Rapilif, Silodal, Urief, Urorec.


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      In Vitro

      In vitro activity: Silodosin shows higher selectivity for the alpha(1A)-AR subtype than tamsulosin hydrochloride, naftopidil or prazosin hydrochloride (affinity is highest for tamsulosin hydrochloride, followed by silodosin, prazosin hydrochloride and naftopidil in that order). Silodosin and tadalafil have synergistic inhibitor effects on nerve-mediated contractions of human and rat isolated prostates in rats.

      In VivoSilodosin strongly antagonizes noradrenaline-induced contractions in rabbit lower urinary tract tissues (including prostate, urethra and bladder trigone, with pA(2) or pKb values of 9.60, 8.71 and 9.35, respectively). Silodosin significantly inhibits the phenylephrine-induced increase in intraurethral pressure (versus the vehicle-treated group) at 12 hours, 18 hours, and 24 hours after its oral administration in rats. Silodosin (0.1-0.3 mg/kg) or prazosin (0.03-0.1 mg/kg) reduces obstruction-induced increases in intraluminal ureter pressures by 21-37% or 18-40% respectively. Silodosin inhibits contractions of the rat and human isolated ureters and has excellent functional selectivity in vivo to relieve pressure-load of the rat obstructed ureter. Silodosin (0.3-300 mg/kg) dose-dependently inhibits the hypogastric nerve stimulation-induced increase in intraurethral pressure (without significant hypotensive effects) in both young and old dogs with benign prostatic hyperplasia. 
      Animal modelRats
      Formulation & Dosage0.1-0.3 mg/kg
      References

      Yakugaku Zasshi. 2006 Mar;126 Spec no.:209-16; Yakugaku Zasshi. 2006 Mar;126 Spec no.:231-6. 

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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