| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
L-803087 targets the somatostatin sst4 receptor, a G protein-coupled receptor. It acts as a potent and highly selective agonist, with a Ki of 0.7 nM for sst4 and over 280-fold selectivity against other somatostatin receptor subtypes. By activating sst4, it modulates neural excitability and synaptic transmission, making it a valuable tool for studying this receptor's role in the central nervous system.
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| ln Vitro |
For cloned human sst1, sst2, sst3, and sst5 receptors, the Ki values of L-803087 are, respectively, 199, 4720, 1280, and 3880 nM [1]. Although the diamine moiety of L-803087 maps to the lysine on the phmacophore, it is unclear how this molecule relates to the Trp and aromatic substituents of the phmacophore. Growth hormone, insulin, and glucagon secretion are not inhibited by L-803087 [1].
In vitro, L-803087 binds to the sst4 receptor with a Ki of 0.7 nM. It shows >280-fold selectivity for sst4 over other somatostatin receptor subtypes. It induces AMPA-mediated hippocampal synaptic responses in vitro, demonstrating its functional activity at the receptor and its utility in studying synaptic modulation. |
| ln Vivo |
In wild-type mice, L-803087 (5 nmol) on average doubled seizure activity. Interestingly, 3 nmol of octreotide can prevent this effect. L-803087 (2 μM) enhanced synaptic responses in hippocampus slices from wild-type mice, while octreotide (2 μM) had no effect on AMPA-mediated synaptic responses [2].
In vivo, L-803087 increases kainate-induced seizures in mice, demonstrating its ability to modulate neural excitability in vivo. Its potent and selective sst4 agonism makes it a valuable tool for studying the role of sst4 in neurological and psychiatric disorders. It is used as a research probe to investigate sst4 receptor function in preclinical models. |
| Enzyme Assay |
In vitro receptor binding assays for L-803087 involve measuring its affinity for somatostatin receptor subtypes. Radioligand binding studies using ¹²⁵I-somatostatin or other selective ligands are performed on membranes from cells expressing sst1-5 receptors. A Ki of 0.7 nM for sst4 is determined. Selectivity is confirmed by testing against other receptor subtypes. Functional assays measure its ability to activate sst4-mediated signaling, such as inhibition of cAMP accumulation.
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| Cell Assay |
For in vitro cell-based assays, cells expressing the sst4 receptor are cultured and treated with L-803087. Receptor activation is measured by quantifying the inhibition of forskolin-stimulated cAMP accumulation. Its effects on neuronal excitability can be assessed in primary neuronal cultures or brain slices by measuring changes in synaptic transmission using electrophysiology.
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| Animal Protocol |
In vivo animal studies with L-803087 are conducted in models of epilepsy and other neurological disorders. The compound is administered systemically, and its effects on seizure susceptibility are measured. Its effects on behavior, cognition, and pain sensitivity can also be assessed. Its ability to modulate neural excitability in vivo makes it a valuable tool for studying sst4 function.
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| ADME/Pharmacokinetics |
L-803087 (CAS: 217480-26-7) is a potent and selective sst4 receptor agonist. Its molecular weight is 485.53 g/mol and its formula is C25H29F2N5O3. It is also known as L-803,087 trifluoroacetate. It is a solid and is typically stored as a powder. It is soluble in DMSO. The compound is a valuable probe for investigating sst4 receptor function.
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| Toxicity/Toxicokinetics |
L-803087 is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a potent sst4 agonist, it may have effects on neural excitability and other physiological processes. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Structure in the first source
L-803087 is a potent and highly selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. It shows over 280-fold selectivity against other somatostatin receptor subtypes and is a valuable probe for studying sst4 receptor function. It is not FDA-approved and is intended for research use only. |
| Molecular Formula |
C₂₅H₂₉F₂N₅O₃
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| Molecular Weight |
485.53
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| Exact Mass |
599.217
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| CAS # |
217480-26-7
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| Related CAS # |
L-803087 TFA;1786412-46-1
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| PubChem CID |
5311374
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
779.7ºC at 760mmHg
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| Flash Point |
425.4ºC
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| Vapour Pressure |
1.34E-25mmHg at 25°C
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| LogP |
5.572
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
35
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| Complexity |
730
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C1C=C(C=C2F)F)C3=CC=CC=C3
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| InChi Key |
OPNMQSFIGUSHDH-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C25H29F2N5O3/c1-35-24(34)20(10-6-12-30-25(28)29)31-21(33)11-5-9-17-18-13-16(26)14-19(27)23(18)32-22(17)15-7-3-2-4-8-15/h2-4,7-8,13-14,20,32H,5-6,9-12H2,1H3,(H,31,33)(H4,28,29,30)/t20-/m0/s1
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| Chemical Name |
methyl (2S)-5-(diaminomethylideneamino)-2-[4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)butanoylamino]pentanoate
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| Synonyms |
L803087; L 803087
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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) |
DMSO : ~250 mg/mL (~514.90 mM)
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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 | 2.0596 mL | 10.2980 mL | 20.5960 mL | |
| 5 mM | 0.4119 mL | 2.0596 mL | 4.1192 mL | |
| 10 mM | 0.2060 mL | 1.0298 mL | 2.0596 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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