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.
Product information
CAS Number: 217480-26-7
Molecular Weight: 599.55
Formula: C27H30F5N5O5
Chemical Name: (Z)-N-[(2S)-5-carbamimidamido-1-methoxy-1-oxopentan-2-yl]-4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)butanimidic acid; trifluoroacetic acid
Smiles: COC(=O)[C@H](CCCNC(N)=N)/N=C(\O)/CCCC1C2C=C(F)C=C(F)C=2NC=1C1C=CC=CC=1.OC(=O)C(F)(F)F
InChiKey: IIRYZHRNVKQVGQ-BDQAORGHSA-N
InChi: InChI=1S/C25H29F2N5O3.C2HF3O2/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;3-2(4,5)1(6)7/h2-4,7-8,13-14,20,32H,5-6,9-12H2,1H3,(H,31,33)(H4,28,29,30);(H,6,7)/t20-;/m0./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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).
Products are for research use only. Not for human use.
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