L-803087 free base · Synonyms: L 803087 · L803087

L-803087 is a potent and selective somatostatin sst4 receptor agonist.

For research use only. Not for human or veterinary use.

Target Somatostatin Receptor

Research area Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

L-803087 structure

CAS No.: 217480-26-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 520.00	BP-01985-100mg	In stock	Get quote
250 mg	USD 940.00	BP-01985-250mg	In stock	Get quote
500 mg	USD 1,498.00	BP-01985-500mg	In stock	Get quote
1 g	Inquire	BP-01985-1g	In stock	Inquire

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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.

Biological activity

In Vitro L-803087 has Ki values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively. 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. 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).

Identifiers

SMILES: N=C(N)NCCC[C@@H](C(OC)=O)NC(CCCC1=C(C2=CC=CC=C2)NC3=C(F)C=C(F)C=C31)=O
InChIKey: OPNMQSFIGUSHDH-FQEVSTJZSA-N

Specifications

MW (average): 485.5263
Formula: C₂₅H₂₉F₂N₅O₃
CAS No.: 217480-26-7
Physical state: Solid
Color: white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 250 mg/mL

Documents

References

[1]. Rohrer SP, et al. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40.

[2]. Moneta D, et al. Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice. Eur J Neurosci. 2002 Sep;16(5):843-9.

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