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- AHU-377(Sacubitril)
AHU-377(Sacubitril)
AHU-377 is an inhibitor of neprilysin with IC50 value of 5nM [1].
AHU-377 and the angiotensin II AT1 receptor antagonist valsartan compose LCZ696 in a 1:1 molar ratio. LCZ696 is an angiotensin receptor neprilysin inhibitor. It can reduce blood pressure and may be a novel drug for the treatment of heart failure. AHU-377 is a prodrug, it can be converted by enzymatic cleavage of the ethyl ester into the active form LBQ657. It is reported that AHU-377(30 and 100 mg/kg, PO) can cause antihypertensive effect in a dose-dependent manner in Dahl-SS rats. But in the DOCA-salt hypertensive rats, it shows a weak reduction [2, 3].
References:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.
[2] Voors AA, Dorhout B, van der Meer P. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacology 2011, 11(Suppl 1):P33.
Physical Appearance | A colorless oil |
Storage | Store at -20°C |
M.Wt | 411.49 |
Cas No. | 149709-62-6 |
Formula | C24H29NO5 |
Synonyms | Sacubitril |
Solubility | ≥41.1 mg/mL in DMSO; ≥21.45 mg/mL in H2O with ultrasonic; ≥26.85 mg/mL in EtOH with ultrasonic |
Chemical Name | 4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoic acid |
SDF | Download SDF |
Canonical SMILES | CCOC(=O)C(C)CC(CC1=CC=C(C=C1)C2=CC=CC=C2)NC(=O)CCC(=O)O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM. | |||||
Targets | neprilysin | |||||
IC50 | 5 nM |
Quality Control & MSDS
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