AHU-377 tris salt
- Sacubitril tris salt
Axon 3856
- Parent CAS: 149709-62-6
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C24H29NO5.C4H11NO3
- MW: 532.63
Description
AHU-377 is a prodrug which is activated in vivo by hydrolytic enzyme esterases to form an active compound LBQ657 that selectively and potently inhibits the enzyme Neprilysin with Ki at low nM. Neprilysin is a protease responsible for the degradation of atrial and brain natriuretic peptides. Inhibition of the enzyme prevents the degradation of natriuretic peptides and activates cGMP signaling pathways that regulate volume and blood pressure. AHU-377 is an investigational antihypertensive drug being studied for use in combination with Valsartan (Axon 3106) in a molar ratio of 1:1.
More Information
| Parent CAS No. | 149709-62-6 |
|---|---|
| Chemical Name | 2-Amino-2-(hydroxymethyl)propane-1,3-diol 4-((2S,4R)-1-(biphenyl-4-yl)-6-methoxy-4-methyl-5-oxohexan-2-ylamino)-4-oxobutanoate |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | N(C(CCC(=O)O)=O)[C@@H](C[C@@H](C)C(=O)COC)CC1C=CC(C2C=CC=CC=2)=CC=1.NC(CO)(CO)CO |&1:8,10,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H29NO5.C4H11NO3/c1-17(22(26)16-30-2)14-21(25-23(27)12-13-24(28)29)15-18-8-10-20(11-9-18)19-6-4-3-5-7-19;5-4(1-6,2-7)3-8/h3-11,17,21H,12-16H2,1-2H3,(H,25,27)(H,28,29);6-8H,1-3,5H2/t17-,21+;/m1./s1 |
| InChiKey | FBMJQYVKCUIZLH-JKSHRDEXSA-N |
| CID | 167530057 |
| Short Description | NEP inhibitor |
References
- LG Hegde et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacol. 2011 Aug 1;11(Suppl 1):P33.
- AA Voors et al. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.
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