2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor
  4. L-803087

L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.

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L-803087 Chemical Structure

L-803087 Chemical Structure

CAS No. : 217480-26-7

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Based on 1 publication(s) in Google Scholar

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L-803087 Related Antibodies

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SSTR1 SSTR2 SSTR3 SSTR5 SSTR4

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Description

L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2].

IC50 & Target

Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)[1]
In Vitro

L-803087 has Ki values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively[1].
L-803087 has a diamine moiety that maps to lysine on the phmacophore, but relation of this molecule to the aromatic and the Trp substituents of the phmacophore are not obvious. L-803087 does not inhibit secretion of growth hormone, insulin, or glucagon[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

L-803087 Related Antibodies
In Vivo

L-803087 (5 nmol) is doubled seizure activity in wild-type mice on average. 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 while facilitation occurred with L-803087 (2 μM)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

485.53

Formula

C25H29F2N5O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

N=C(N)NCCC[C@@H](C(OC)=O)NC(CCCC1=C(C2=CC=CC=C2)NC3=C1C=C(F)C=C3F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (514.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0596 mL 10.2980 mL 20.5961 mL
5 mM 0.4119 mL 2.0596 mL 4.1192 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: ≥98.0%

COA (248 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0596 mL 10.2980 mL 20.5960 mL 51.4901 mL
5 mM 0.4119 mL 2.0596 mL 4.1192 mL 10.2980 mL
10 mM 0.2060 mL 1.0298 mL 2.0596 mL 5.1490 mL
15 mM 0.1373 mL 0.6865 mL 1.3731 mL 3.4327 mL
20 mM 0.1030 mL 0.5149 mL 1.0298 mL 2.5745 mL
25 mM 0.0824 mL 0.4119 mL 0.8238 mL 2.0596 mL
30 mM 0.0687 mL 0.3433 mL 0.6865 mL 1.7163 mL
40 mM 0.0515 mL 0.2575 mL 0.5149 mL 1.2873 mL
50 mM 0.0412 mL 0.2060 mL 0.4119 mL 1.0298 mL
60 mM 0.0343 mL 0.1716 mL 0.3433 mL 0.8582 mL
80 mM 0.0257 mL 0.1287 mL 0.2575 mL 0.6436 mL
100 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5149 mL
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L-803087 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-803087217480-26-7L803087L 803087Somatostatin ReceptorSSTRsSSTRsst4seizureshippocampalsynapticAMPAdiamineInhibitorinhibitorinhibit

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