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L-803087

Name: L-803087
Brand: TargetMol
SKU: T11800
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11800Cas No. 217480-26-7

L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors. L-803087 induces AMPA-mediated synaptic responses in the hippocampus in vitro and increases seizures in alginate-induced seizure-busting mice in vivo.

L-803087

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Purity: 99.37%

Catalog No. T11800Cas No. 217480-26-7

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	-	In Stock
5 mg	$121	-	In Stock
10 mg	$195	-	In Stock
25 mg	$407	-	In Stock
50 mg	$651	-	In Stock
100 mg	$1,030	-	In Stock
200 mg	$1,370	-	In Stock
1 mL x 10 mM (in DMSO)	$135	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.37%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors. L-803087 induces AMPA-mediated synaptic responses in the hippocampus in vitro and increases seizures in alginate-induced seizure-busting mice in vivo.
Targets&IC50	SST4 receptor:0.7 nM (ki), SST5 receptor:3880 nM (ki), SST3 receptor:1280 nM (ki), SST1 receptor:199 nM (ki), SST2 receptor:4720 nM (ki)
In vitro	L-803087 has Ki values of 199, 4720, 1280, and 3880 nM for cloned human sst1, sst2, sst3, and sst5 receptors, respectively[2]. The molecule L-803087 features a diamine moiety mapping to lysine on the pharmacophore. However, the relationship of this molecule to the aromatic and Trp substituents of the pharmacophore is not apparent. L-803087 does not inhibit the secretion of growth hormone, insulin, or glucagon[2].
In vivo	In wild-type mice, the administration of L-803087 (5 nmol) on average doubles seizure activity. Interestingly, this effect is blocked by 3 nmol Octreotide. In hippocampal slices from wild-type mice, Octreotide (2 μM) does not modify AMPA-mediated synaptic responses, whereas facilitation occurs with L-803087 (2 μM)[1].

Chemical Properties

Molecular Weight	485.53
Formula	C₂₅H₂₉F₂N₅O₃
Cas No.	217480-26-7
Smiles	COC(=O)[C@H](CCCNC(N)=N)NC(=O)CCCc1c([nH]c2c(F)cc(F)cc12)-c1ccccc1
Relative Density.	1.33 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 55 mg/mL (113.28 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0596 mL	10.2980 mL	20.5960 mL	102.9802 mL
5 mM	0.4119 mL	2.0596 mL	4.1192 mL	20.5960 mL
10 mM	0.2060 mL	1.0298 mL	2.0596 mL	10.2980 mL
20 mM	0.1030 mL	0.5149 mL	1.0298 mL	5.1490 mL
50 mM	0.0412 mL	0.2060 mL	0.4119 mL	2.0596 mL
100 mM	0.0206 mL	0.1030 mL	0.2060 mL	1.0298 mL

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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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc