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| Targets |
LHW090-A7 targets neutral endopeptidase (NEP), a membrane-bound zinc metallopeptidase. NEP is responsible for the cleavage and inactivation of a wide range of peptide hormones, including enkephalins, substance P, and atrial natriuretic peptides (ANP). By inhibiting NEP, LHW090-A7 prevents the degradation of these peptides, leading to an increase in their active concentrations. For ANP, this results in natriuretic and diuretic effects, making NEP inhibitors a target for the treatment of hypertension and heart failure.
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| ln Vitro |
In vitro, LHW090-A7's activity is measured by its ability to inhibit the enzymatic activity of neutral endopeptidase. The enzyme is incubated with a substrate, such as a fluorogenic peptide, in a buffer system. LHW090-A7 is added at various concentrations, and the enzymatic activity is measured by the release of a fluorescent signal. The compound's IC50, the concentration required to inhibit 50% of the enzyme's activity, is determined from a dose-response curve.
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| ln Vivo |
In vivo, LHW090-A7 is expected to induce natriuretic and diuretic effects by inhibiting NEP. This leads to an increase in plasma levels of endogenous atrial natriuretic peptides, which promote sodium and water excretion. These effects make NEP inhibitors like LHW090-A7 promising candidates for the treatment of hypertension, heart failure, and other cardiovascular diseases.
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| Enzyme Assay |
Non-cell-based enzyme assays for LHW090-A7 typically involve the use of purified NEP enzyme. The enzyme is incubated with a fluorogenic substrate, such as Mca-RPPGFSAFK(Dnp)-OH, in a buffer system. LHW090-A7 is added at various concentrations, and the increase in fluorescence, which is proportional to enzyme activity, is measured over time. The compound's IC50 is determined from a dose-response curve.
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| Cell Assay |
Cellular assays for LHW090-A7 are not extensively detailed in the provided search results. However, they could be performed using cells that express NEP, such as renal epithelial cells. The cells would be treated with the compound, and the degradation of a peptide substrate (e.g., ANP) would be measured. The compound's ability to inhibit the degradation of the peptide would be quantified.
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| Animal Protocol |
In vivo animal models for NEP inhibitors like LHW090-A7 typically involve the use of normotensive or hypertensive rats. The compound is administered orally or intravenously, and its effect on urinary sodium excretion, urine volume, and blood pressure is measured. These studies are crucial for establishing the in vivo efficacy and dose-response relationship of the compound.
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| ADME/Pharmacokinetics |
LHW090-A7 has a molecular weight of 375.85 g/mol and a molecular formula of C20H22ClNO4. It is a small molecule that is likely to be orally bioavailable. Detailed PK parameters such as half-life, Cmax, and bioavailability are not extensively detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for LHW090-A7 are not provided in the search results. As an enzyme inhibitor, its safety profile would be a key consideration. Off-target effects on other peptidases could lead to toxicity. The compound is intended for research use only and is not for human consumption.
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| Additional Infomation |
LHW090-A7 is a neutral endopeptidase (NEP) inhibitor. By inhibiting NEP, it increases plasma levels of atrial natriuretic peptides, inducing natriuretic and diuretic effects. It has a molecular weight of 375.85 g/mol and a molecular formula of C20H22ClNO4. It has the CAS number 1308256-94-1 and is supplied for research purposes as a potential therapeutic agent for cardiovascular diseases.
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| Molecular Formula |
C20H22CLNO4
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| Molecular Weight |
375.849
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| Exact Mass |
375.123
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| CAS # |
1308256-94-1
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| Related CAS # |
1308256-94-1;
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| PubChem CID |
58280516
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
528.2±50.0 °C at 760 mmHg
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| Flash Point |
273.2±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.566
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| LogP |
5.18
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
26
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| Complexity |
465
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC1=CC=CC(=C1)C1C=CC(=CC=1)C[C@@H](C(=O)O)NC(C(=O)OCC)C
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| InChi Key |
PWYAUIUPDMSWJH-UGSOOPFHSA-N
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| InChi Code |
InChI=1S/C20H22ClNO4/c1-3-26-20(25)13(2)22-18(19(23)24)11-14-7-9-15(10-8-14)16-5-4-6-17(21)12-16/h4-10,12-13,18,22H,3,11H2,1-2H3,(H,23,24)/t13-,18-/m0/s1
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| Chemical Name |
(2S)-3-[4-(3-Chlorophenyl)phenyl]-2-[[(2S)-1-ethoxy-1-oxopropan-2-yl]amino]propanoic acid
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| Synonyms |
LHW090-A7 LHW090 A7 LHW090A7 LHW090 Analog 7
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6606 mL | 13.3032 mL | 26.6064 mL | |
| 5 mM | 0.5321 mL | 2.6606 mL | 5.3213 mL | |
| 10 mM | 0.2661 mL | 1.3303 mL | 2.6606 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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