| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| ln Vitro |
Sacubitrilat (LBQ657) has a distinct stereocenter and is a single diastereomer. Sacubitrilat exhibits a high inhibitory efficacy of 5 nM upon binding to the active site of NEP via a complicated response network including all of the compound's functional groups [1].
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|---|---|
| ln Vivo |
Following a single sidewall dosage of LCZ696 at 400 or 1200 mg while fasting, the pharmacokinetics of Sacubitrilat, Sacubitrilat la (LBQ657), and the insecticide Sartan are compiled. Sacubitril's mean intraperitoneal concentration rose quickly; its median Tmax for the 400 mg and 1200 mg doses was 0.52 hours, and its Tmax for Sacubitril was 1.05 hours. Sacubitril's Tmax values were 2.07 and 3.05 hours, respectively. The median Tmax for brasartan for the LCZ696 400 mg and 1200 mg dosages was 2.07 hours. The increase in Sacubitril's Cmax was dose-proportional, and there was a less than proportional increase in Sacubitril's Cmax between doses. When it comes to sacubitril and sacubitrilat, arithmetic tools AUC0-24 h and AUClast grew about dose-proportionally, but they did not grow as much when it came to sartan [2].
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| References | |
| Additional Infomation |
A metabolite of LCZ696 with neprilysin inhibitory activity.
Sacubitrilat is a Neprilysin Inhibitor. The mechanism of action of sacubitrilat is as a Neprilysin Inhibitor. |
| Molecular Formula |
C22H25NO5
|
|---|---|
| Molecular Weight |
383.4376
|
| Exact Mass |
383.173
|
| CAS # |
149709-44-4
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| Related CAS # |
Sacubitrilat-d4
|
| PubChem CID |
10430040
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.196
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
28
|
| Complexity |
521
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C[C@H](C[C@@H](CC1=CC=C(C=C1)C2=CC=CC=C2)NC(=O)CCC(=O)O)C(=O)O
|
| InChi Key |
DOBNVUFHFMVMDB-BEFAXECRSA-N
|
| InChi Code |
InChI=1S/C22H25NO5/c1-15(22(27)28)13-19(23-20(24)11-12-21(25)26)14-16-7-9-18(10-8-16)17-5-3-2-4-6-17/h2-10,15,19H,11-14H2,1H3,(H,23,24)(H,25,26)(H,27,28)/t15-,19+/m1/s1
|
| Chemical Name |
(2R,4S)-4-(3-carboxypropanoylamino)-2-methyl-5-(4-phenylphenyl)pentanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~260.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6080 mL | 13.0398 mL | 26.0797 mL | |
| 5 mM | 0.5216 mL | 2.6080 mL | 5.2159 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6080 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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