Avanafil , ≥99% , 330784-47-9

Synonym(s):
(S)-2-(2-Hydroxymethyl-1-pyrrolidinyl)-4-(3-chloro-4-methoxybenzylamino)-5-[N-(2-pyrimidinylmethyl)carbamoyl]pyrimidine;(S)-4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide;4-[[(3-Chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide

CAS NO.：330784-47-9

Empirical Formula: C23H26ClN7O3

Molecular Weight: 483.95

MDL number: MFCD11977961

EINECS: 000-000-0

PRODUCT Properties

• Melting point: 150-152°C
• Density: 1.372
• storage temp.: Sealed in dry,Store in freezer, under -20°C
• solubility: DMSO (Slightly), Methanol (Slightly, Heated)
• form: Solid
• pka: 11.84±0.46(Predicted)
• color: White to Off-White
• InChIKey: WEAJZXNPAWBCOA-INIZCTEOSA-N
• SMILES: C1(N2CCC[C@H]2CO)=NC=C(C(NCC2=NC=CC=N2)=O)C(NCC2=CC=C(OC)C(Cl)=C2)=N1

Description and Uses

Avanafil (Zepeed) was approved by the Korean Health Ministry for the treatment of erectile dysfunction (ED) in August 2011. Avanafil is a highly selective type 5 phosphodiesterase (PDE5) inhibitor. Avanafil is reported to be the most selective PDE5 inhibitor on the market. The onset of Tmax and half-life also varies among the marketed PDE5 inhibitors. Sildenafil has a T_max at 1 h and a half-life of 3–5 h. Vardenafil is somewhat similar with a T_max of 0.6 h and a half-life of 4–6 h. Tadalafil has the longest half-life among the marketed drugs with a half-life of 17 h. Avanafil has a fast onset of action reaching T_max in 0.6 h with a half-life of 1.2 h. A synthesis of avanafil (TA-1790) is described in the patent literature. The main elimination route of avanafil is through the bile and feces. Avanafil was also found to be reabsorbed through enterohepatic recirculation.

A phosphodiesterase (PDE5) inhibitor, used to treat erectile dysfunction.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338
• HS Code: 29339900