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L-803087 TFA
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Catalog No. T39207Cas No. 1786412-46-1
L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.
L-803087 TFA
Copy Product Info😃Good
Catalog No. T39207Cas No. 1786412-46-1
L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 100 mg | Inquiry | Inquiry | Inquiry | |
| 500 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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| Description | L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice. |
| Targets&IC50 | SST5 receptor:3880 nM (Ki), SST4 receptor:0.7 nM (Ki), SST1 receptor:199 nM (Ki), SST2 receptor:4720 nM (Ki), SST3 receptor:1280 nM (Ki) |
| In vitro | L-803087 exhibits affinity for cloned human sst1, sst2, sst3, and sst5 receptors with K_i values of 199, 4720, 1280, and 3880 nM, respectively[1]. It features a diamine moiety aligned with lysine on the pharmacophore; however, the connection between this molecule and the pharmacophore's aromatic and Trp (tryptophan) substituents remains unclear. Additionally, L-803087 does not suppress the secretion of growth hormone, insulin, or glucagon[1]. |
| In vivo | Administering 5 nmol of L-803087 on average doubles seizure activity in wild-type mice, an effect that is inhibited by 3 nmol of Octreotide. Additionally, in hippocampal slices from wild-type mice, 2 μM Octreotide does not alter AMPA-mediated synaptic responses, whereas 2 μM L-803087 induces facilitation[2]. |
| Molecular Weight | 599.55 |
| Formula | C27H30F5N5O5 |
| Cas No. | 1786412-46-1 |
| Smiles | OC(=O)C(F)(F)F.COC(=O)[C@H](CCCNC(N)=N)NC(=O)CCCc1c([nH]c2c(F)cc(F)cc12)-c1ccccc1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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