| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
LAS38096 targets the enzyme neutral endopeptidase 24.11 (NEP, neprilysin, EC 3.4.24.11). NEP is a membrane-bound zinc metalloprotease widely distributed in various tissues, including the kidney, lung, and brain. Its primary function is the cleavage and inactivation of a range of peptide hormones. By binding to the active site of NEP, LAS38096 inhibits its enzymatic activity, preventing the degradation of its substrates. The inhibition is typically competitive and reversible. This leads to increased levels of natriuretic peptides, which exert beneficial effects on cardiovascular and renal function.
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| ln Vitro |
In vitro, LAS38096's activity is assessed by its ability to inhibit the enzymatic activity of purified NEP. The enzyme is incubated with a fluorogenic or chromogenic substrate in the presence of varying concentrations of the compound. The rate of substrate cleavage is measured, and the concentration required to inhibit 50% of the enzyme's activity (IC₅₀) is determined. Its selectivity for NEP over other metalloproteases, such as ACE, is also evaluated. Detailed IC₅₀ values are not extensively provided in the referenced sources.
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| ln Vivo |
In vivo, LAS38096 is expected to induce natriuretic and diuretic effects by inhibiting NEP and thereby increasing the levels of endogenous natriuretic peptides. This leads to vasodilation, reduced blood pressure, and increased sodium and water excretion. These effects make NEP inhibitors like LAS38096 promising candidates for the treatment of hypertension and heart failure. Detailed in vivo data from specific animal models are not extensively provided in the referenced sources.
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| Enzyme Assay |
Non-cell-based enzyme assays for LAS38096 typically involve the use of purified NEP enzyme. The enzyme is incubated with a fluorogenic substrate, such as Mca-RPPGFSAFK(Dnp)-OH, in a suitable buffer. LAS38096 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. Assays for selectivity against other peptidases, such as ACE, are also performed.
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| Cell Assay |
Cellular assays for LAS38096 are not typical, as its target is a membrane-bound enzyme that is often studied in cell-free systems. However, assays using cells that express NEP, such as renal epithelial cells, can be performed. Cells are treated with the compound, and the degradation of a peptide substrate (e.g., ANP) is measured. The compound's ability to inhibit the degradation of the peptide is quantified.
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| Animal Protocol |
In vivo animal models for NEP inhibitors like LAS38096 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 |
LAS38096 has a molecular weight of 427.47 g/mol. Its CAS number is 851371-22-7. The compound is a small molecule that is likely to be orally bioavailable. It is supplied as a solid for research use. Purity is typically ≥98%. Storage conditions: -20°C. Detailed PK parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for LAS38096 are not extensively provided in the referenced sources. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
LAS38096 is a neutral endopeptidase (NEP) inhibitor. By inhibiting NEP, it increases the levels of natriuretic peptides, inducing natriuretic and diuretic effects. It is a research compound with potential applications in cardiovascular diseases. Its CAS number is 851371-22-7.
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| Molecular Formula |
C17H12N6O
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|---|---|
| Molecular Weight |
316.32
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| Exact Mass |
316.107
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| CAS # |
851371-22-7
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| PubChem CID |
11716665
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.405
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
397
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C2=CN=C(NC3=CC=CN=C3)N=C2C4=CC=CO4)=NC=NC=C1
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| InChi Key |
YRPIMMMBNUUYLG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12N6O/c1-3-12(9-18-6-1)22-17-20-10-13(14-5-7-19-11-21-14)16(23-17)15-4-2-8-24-15/h1-11H,(H,20,22,23)
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| Chemical Name |
4-(furan-2-yl)-N-pyridin-3-yl-5-pyrimidin-4-ylpyrimidin-2-amine
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| Synonyms |
LAS-38096; LAS 38096; LAS38096
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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 | 3.1614 mL | 15.8068 mL | 31.6136 mL | |
| 5 mM | 0.6323 mL | 3.1614 mL | 6.3227 mL | |
| 10 mM | 0.3161 mL | 1.5807 mL | 3.1614 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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