AHU-377(Sacubitril) (Synonyms: Sacubitril) |
رقم الكتالوجGC10146 |
AHU-377 (Sacubitril) (AHU-377) هو مثبط قوي وفعال عن طريق الفم (neprilysin) مع IC50 من 5 نانومتر.
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Cas No.: 149709-62-6
Sample solution is provided at 25 µL, 10mM.
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.
Cas No. | 149709-62-6 | SDF | |
المرادفات | Sacubitril | ||
Chemical Name | 4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoic acid | ||
Canonical SMILES | CCOC(=O)C(C)CC(CC1=CC=C(C=C1)C2=CC=CC=C2)NC(=O)CCC(=O)O | ||
Formula | C24H29NO5 | M.Wt | 411.49 |
الذوبان | ≥ 41.1mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.4302 mL | 12.151 mL | 24.3019 mL |
5 mM | 0.486 mL | 2.4302 mL | 4.8604 mL |
10 mM | 0.243 mL | 1.2151 mL | 2.4302 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5
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