| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
L-817,818 targets the somatostatin subtype 5 (sst5) receptor, a G protein-coupled receptor that is activated by the peptide hormone somatostatin. It acts as a potent agonist, with a Ki of 0.4 nM for the human sst5 receptor. The compound shows selectivity for sst5 over other somatostatin receptor subtypes, with Ki values of 3.3 nM for sst1, 52 nM for sst2, 64 nM for sst3, and 82 nM for sst4. Activation of sst5 by L-817,818 inhibits adenylyl cyclase and modulates various cellular functions.
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| ln Vitro |
In vitro, L-817,818 binds to the human sst5 receptor with high affinity (Ki = 0.4 nM) and shows selectivity over other somatostatin receptor subtypes. The compound activates sst5-mediated signaling, as measured by inhibition of cAMP accumulation or other downstream readouts. L-817,818 is a non-peptide agonist that was identified from combinatorial libraries, making it a valuable tool for studying sst5 receptor pharmacology.
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| ln Vivo |
In vivo, L-817,818 has been studied for its potential in endocrine and metabolic research. As an sst5 agonist, it may modulate growth hormone secretion, insulin release, and other hormonal functions. However, specific in vivo efficacy data are limited in the available literature. L-817,818 is primarily used as a research tool for studying somatostatin receptor pharmacology.
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| Enzyme Assay |
The non-cellular assay for L-817,818 involves measuring its binding affinity for somatostatin receptor subtypes using radioligand binding assays. Membrane preparations from cells expressing human sst1-sst5 receptors are incubated with a radiolabeled somatostatin receptor ligand (such as [¹²⁵I]-Tyr¹¹-somatostatin-14) and varying concentrations of L-817,818. The inhibition of radioligand binding is measured, and the Ki is determined from competition curves.
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| Cell Assay |
The cellular assay for L-817,818 involves treating cells expressing the sst5 receptor with the compound and measuring its effects on receptor-mediated signaling. Cells are pre-incubated with forskolin to stimulate adenylyl cyclase, and L-817,818 is added at various concentrations. The inhibition of cAMP accumulation is measured using a competitive immunoassay. The EC50 is determined from concentration-response curves.
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| Animal Protocol |
In the in vivo efficacy study, L-817,818 is administered to animal models to assess its effects on hormone secretion and metabolism. The compound is typically administered by injection or oral gavage. Blood samples are collected for measurement of growth hormone, insulin, or other hormones. However, specific published protocols for L-817,818 are limited.
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| ADME/Pharmacokinetics |
L-817,818 has a molecular weight of 536.66 and a molecular formula of C₃₃H₃₆N₄O₃. The compound is a non-peptide somatostatin receptor agonist. It should be stored as a powder at -20°C, protected from light and moisture. L-817,818 should be handled with appropriate laboratory safety precautions. The compound is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
The toxicological profile of L-817,818 has not been extensively characterized in the published literature. As an sst5 agonist, it may have effects on hormone secretion and metabolism. Comprehensive toxicology data are limited, and L-817,818 is not approved for clinical use. The compound should be handled with appropriate laboratory safety precautions.
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| References | |
| Additional Infomation |
Somatostatin 5 receptor agonists
L-817,818 is a potent and selective non-peptide somatostatin sst5 receptor agonist that has been used as a research tool to study somatostatin receptor pharmacology. Its high affinity for sst5 (Ki = 0.4 nM) and selectivity over other somatostatin receptor subtypes make it a valuable tool for investigating sst5-specific functions. L-817,818 was identified from combinatorial libraries constructed on the basis of molecular modeling of known peptide agonists. The compound is not approved for clinical use and is strictly a research tool. |
| Molecular Formula |
C33H36N4O3
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|---|---|
| Molecular Weight |
536.68
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| Exact Mass |
536.279
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| CAS # |
217480-27-8
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| PubChem CID |
9937014
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| Appearance |
White to off-white solid powder
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| LogP |
6.979
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
40
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| Complexity |
839
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@H](COC(=O)[C@@H](CCCCN)NC(=O)CC1=C(NC2=C1C=CC3=CC=CC=C32)C4=CC5=CC=CC=C5C=C4)N
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| InChi Key |
NFVRGDRCCNEGBS-KCWXNJEJSA-N
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| InChi Code |
InChI=1S/C33H36N4O3/c1-21(35)20-40-33(39)29(12-6-7-17-34)36-30(38)19-28-27-16-15-23-9-4-5-11-26(23)32(27)37-31(28)25-14-13-22-8-2-3-10-24(22)18-25/h2-5,8-11,13-16,18,21,29,37H,6-7,12,17,19-20,34-35H2,1H3,(H,36,38)/t21-,29+/m0/s1
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| Chemical Name |
[(2S)-2-aminopropyl] (2R)-6-amino-2-[[2-(2-naphthalen-2-yl-1H-benzo[g]indol-3-yl)acetyl]amino]hexanoate
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| Synonyms |
L817,818 L 817,818 L-817,818
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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 | 1.8633 mL | 9.3165 mL | 18.6331 mL | |
| 5 mM | 0.3727 mL | 1.8633 mL | 3.7266 mL | |
| 10 mM | 0.1863 mL | 0.9317 mL | 1.8633 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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