Rapaflo Inhibitor CAS No. 160970-54-7

Cat. No.	Name	Size	Price	Add Cart
KI0860	Rapaflo	500 mg	$418
KI0860	Rapaflo	1 g	$530

Chemical Characteristic

Product Name	Rapaflo
Synonyms	Silodosin,Silodyx, Rapilif, Silodal, Urief, KMD3213
CAS No.	160970-54-7
Molecular Weight	495.53
Formula	C₂₅H₃₂F₃N₃O₄
Chemical Structure

Biological activities

Rapaflo is a novel selective α1A-adrenoceptor selective antagonist. Rapaflo is used to treat benign prostatic hyperplasia.^[1] Rapaflo significantly improves lower urinary tract symptoms associated with benign prostatic hyperplasia.^[2] Rapaflo decreases neointima growth by approximately 30 and 46% at the two doses of 12.8 and 32 µg/kg, respectively.^[3] Rapaflo inhibits norepinephrine-induced increases in intracellular Ca²⁺ concentrations in α1A -AR-expressing Chinese hamster ovary cells with an IC50 of 0.32 nM. However, rapaflo has a much weaker inhibitory effect on the alpha 1b- and alpha 1d-ARs.^[4] Oral administration of rapaflo (0.2閳?0.2 µmol/kg, 0.5 hour) dose-dependently decreases [³H]prazosin binding sites (Bmax) in the prostate (42閳?4%) and submaxillary gland (54閳?8%) compared with the control value.^[5] Rapaflo doesn閳ユ獩 reduce the noradrenaline content in the five rat tissues. ^[6]

Protocols

In vivo: Rapaflo is dissolved in saline.^[6]

References

[1] Yoshida M, et al. Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia. Expert Opin Investig Drugs. 2007, 16(12): 1955-1965. 閵嗏偓閵嗏偓 [2] Guay David RP, et al. Silodosin: an orally active selective α1-adrenoceptor antagonist for benign prostatic hyperplasia. 2009, 5(4): 459-473. 閵嗏偓閵嗏偓 [3] Teeters JC, et al. Systemic alpha 1A-adrenoceptor antagonist inhibits neointimal growth after balloon injury of rat carotid artery. Am J Physiol Heart Circ Physiol. 2003, 284(1): H385-H392. 閵嗏偓閵嗏偓 [4] Shibata K, et al. KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues. Mol Pharmacol. 1995, 48(2): 250-258. 閵嗏偓閵嗏偓 [5] Okura T, et al. Selective and sustained occupancy of prostatic alpha1-adrenoceptors by oral administration of KMD-3213 and its plasma concentration in rats. J Pharm Pharmacol. 2002, 54(7): 975-982. 閵嗏偓閵嗏偓 [6] Zhang L, et al. Alpha-1 adrenoceptor up-regulation induced by prazosin but not KMD-3213 or reserpine in rats. Br J Pharmacol. 2002, 135(7): 1757-1764. 閵嗏偓閵嗏偓

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