Date published: 2026-5-31

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AHU 377 (CAS 149709-62-6)

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Alternate Names:
Sacubitril; AHU377; AHU-377
Application:
AHU 377 is an inhibitor of neprilysin with IC50 value of 5 nM.
CAS Number:
149709-62-6
Purity:
≥98%
Molecular Weight:
411.49
Molecular Formula:
C24H29NO5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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AHU 377 is an inhibitor of neprilysin with IC50 value of 5 nM. 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. It combines two drugs, sacubitril (a neprilysin inhibitor) and valsartan (an angiotensin receptor blocker). Neprilysin is an enzyme that breaks down natriuretic peptides, which play a role in regulating sodium and water balance in the body. By inhibiting neprilysin, AHU 377 increases the concentration of natriuretic peptides, leading to increased sodium and water excretion and a decrease in blood volume and pressure.


AHU 377 (CAS 149709-62-6) References

  1. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi).  |  Gu, J., et al. 2010. J Clin Pharmacol. 50: 401-14. PMID: 19934029
  2. Hypertension: LCZ696, a novel dual inhibitor of neprilysin and the angiotensin II receptor, shows promise in phase II trial.  |  Lucchese, B. 2010. Nat Rev Nephrol. 6: 383. PMID: 20597156
  3. Combination angiotensin receptor blocker-neutral endopeptidase inhibitor provides additive blood pressure reduction over angiotensin receptor blocker alone.  |  Bloch, MJ. and Basile, JN. 2010. J Clin Hypertens (Greenwich). 12: 809-12. PMID: 21029344
  4. Combined neprilysin and renin-angiotensin system inhibition for the treatment of heart failure.  |  Vardeny, O., et al. 2014. JACC Heart Fail. 2: 663-70. PMID: 25306450
  5. Neprilysin, cardiovascular, and Alzheimer's diseases: the therapeutic split?  |  Vodovar, N., et al. 2015. Eur Heart J. 36: 902-5. PMID: 25636748
  6. Pharmacokinetic drug-drug interaction assessment between LCZ696, an angiotensin receptor neprilysin inhibitor, and hydrochlorothiazide, amlodipine, or carvedilol.  |  Hsiao, HL., et al. 2015. Clin Pharmacol Drug Dev. 4: 407-17. PMID: 27137712
  7. Pharmacokinetic, pharmacodynamic, and antihypertensive effects of the neprilysin inhibitor LCZ-696: sacubitril/valsartan.  |  Chrysant, SG. 2017. J Am Soc Hypertens. 11: 461-468. PMID: 28652105
  8. The Sacubitril/Valsartan, a First-in-Class, Angiotensin Receptor Neprilysin Inhibitor (ARNI): Potential Uses in Hypertension, Heart Failure, and Beyond.  |  Kario, K. 2018. Curr Cardiol Rep. 20: 5. PMID: 29374807
  9. AHU377+Valsartan (LCZ696) Modulates Renin-Angiotensin System (RAS) in the Cardiac of Female Spontaneously Hypertensive Rats Compared With Valsartan.  |  Zhao, Y., et al. 2019. J Cardiovasc Pharmacol Ther. 24: 450-459. PMID: 31023080
  10. ARNI in cardiovascular disease: current evidence and future perspectives.  |  Kuchulakanti, PK. 2020. Future Cardiol. 16: 505-515. PMID: 32319309
  11. Angiotensin receptor-neprilysin inhibitors: Comprehensive review and implications in hypertension treatment.  |  Yamamoto, K. and Rakugi, H. 2021. Hypertens Res. 44: 1239-1250. PMID: 34290389
  12. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension  |  Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi, Russell Araki, Jennifer Villarreal, Glenmar Obedencio, Anne Kanta, Erik Sandvick, Craig Hill, Kevin Dement, Uwe Klein, Donavon McConn, William Martin & Sharath S Hegde. 2011. BMC Pharmacology. 11.
  13. A1435 Effects of valsartan + AHU377 (LCZ696) attenuation of fibrosis in cardiac and vagina compared with valsartan in female spontaneously hypertensive rat  |  Yang, Zhao; Ma, Ruixin; Yu, Xiaorong; Li, Ningyin; Zhao, Xu; Zhang, Panpan; Yu, Heng; Liang, Wei; Zhang, Xiaowei; Yuan, Ruowen; Yu, Jing. 2018. Journal of Hypertension. 36.
  14. Neprilysin Inhibition by an Antisense Oligonucleotide (ASO) Ameliorates Kidney Damage in a Salt-induced Rat Chronic Kidney Disease Model  |  Steve Ting-Yuan Yeh, Adam Mullick, Carol Kuo, Mark Graham, Rosanne Crooke. 2018. The FASEB. 32: lb353-lb353.

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AHU 377, 5 mg

sc-492600
5 mg
$235.00