Tadalafil Inhibitor CAS No. 171596-29-5

Cat. No.	Name	Size	Price
KI0953	Tadalafil	50 mg	$176
	Tadalafil	100 mg	$272
	Tadalafil	500 mg	$1072

Chemical Characteristic

Product Name	Tadalafil
Synonyms	Cialis
CAS No.	171596-29-5
Molecular Weight	389.4
Formula	C₂₂H₁₉N₃O₄
Chemical Name	(6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
Smiles	[nH]1c2c(c3ccccc13)C[C@H]1N([C@H]2c2cc3OCOc3cc2)C(=O)CN(C1=O)C
Chemical Structure
Documents	HNMR COA HPLC MS

Biological activities

Tadalafil is a selective phosphodiesterase-5 (PDE-5) inhibitor. Tadalafil competitively inhibits cGMP hydrolysis, fostering cGMP accumulation and relaxation of vascular smooth muscle. Tadalafil inhibits PDE-5 with an IC50 of 1.8 nM and bounds to PDE5 with a stoichiometry of 0.68 moL/subunit. Biochemical potencies (affinities) of tadalafil for PDE5 determined by KD (isotherm), KD (dissociationrate), and KD (1/2 EC50) are 2.4, 1.9 and 2.7 nM, respectively.^[1] Tadalafil is extremely selective for PDE5, but also potently inhibits PDE11, an enzyme with unknown physiological function, with an IC50 of 37 nM.^[2] Tadalafil is broken down mainly via cytochrome P450 CYP3A4. Besides, tadalafil potentiates the hypotensive and anticoagulant effect of nitrates and NO donors.^[3] Oral administration of tadalafil (10 mg/kg) 2 hours before 30 minute-coronary artery occlusion results in a smaller infarct size (42%) as compared with the vehicle-treated animals (54%).^[4]

References

[1] Blount MA, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004, 66 (1): 144-152. [2] Bischoff E, et al. Potency, selectivity, and consequences of nonselectivity of PDE inhibition. Int J Impot Res. 2004, 16: S11-14. [3] Gresser U, et al. Erectile dysfunction: comparison of efficacy and side effects of the PDE-5 inhibitors sildenafil, vardenafil and tadalafil--review of the literature. Eur J Med Res. 2002, 7 (10): 435-446. [4] Kukreja R, et al. Anti-ischemic effects of sildenafil, vardenafil and tadalafil in heart. Int J Impot Res. 2007, 19 (2): 226-227.

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