L-803087 trifluoroacetate | CAS# 217480-26-7 (TFA) | Somatostatin sst4 receptor agonist

MedKoo Cat#: 574369 | Name: L-803087 trifluoroacetate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

L-803087 is a somatostatin sst4 receptor agonist.

Chemical Structure

L-803087 trifluoroacetate

CAS#217480-26-7 (TFA)

Theoretical Analysis

MedKoo Cat#: 574369

Name: L-803087 trifluoroacetate

CAS#: 217480-26-7 (TFA)

Chemical Formula: C27H30F5N5O5

Exact Mass: 599.2167

Molecular Weight: 599.56

Elemental Analysis: C, 54.09; H, 5.04; F, 15.84; N, 11.68; O, 13.34

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 335.00	2 Weeks

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Synonym

L-803087 trifluoroacetate; L803087 trifluoroacetate; L 803087 trifluoroacetate; L-803087 TFA

IUPAC/Chemical Name

N2-[4-(5,7-Difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-L-arginine methyl ester c

InChi Key

IIRYZHRNVKQVGQ-BDQAORGHSA-N

InChi Code

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

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

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 Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM.

In vitro activity:

Whole cell patch clamp recordings were made on isolated immunopanned RGCs using barium as a charge carrier to isolate Ica (calcium channel currents). Application of the selective sst4 agonist, L-803 (10 nM), reduced ICa by 41.2%. Reference: Channels (Austin). 2014;8(6):519-27. https://pubmed.ncbi.nlm.nih.gov/25483286/

In vivo activity:

L-803087 (5 nmol), a selective sst4 receptor agonist, doubled seizure activity in wild-type mice on average. Reference: Eur J Neurosci. 2002 Sep;16(5):843-9. https://pubmed.ncbi.nlm.nih.gov/12372020/

Preparing Stock Solutions

The following data is based on the product molecular weight 599.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Farrell SR, Rankin DR, Brecha NC, Barnes S. Somatostatin receptor subtype 4 modulates L-type calcium channels via Gβγ and PKC signaling in rat retinal ganglion cells. Channels (Austin). 2014;8(6):519-27. doi: 10.4161/19336950.2014.967623. Erratum in: Channels (Austin). 2015;9(1):56-7. PMID: 25483286; PMCID: PMC4594562. 2. Cammalleri M, Martini D, Timperio AM, Bagnoli P. Functional effects of somatostatin receptor 1 activation on synaptic transmission in the mouse hippocampus. J Neurochem. 2009 Dec;111(6):1466-77. doi: 10.1111/j.1471-4159.2009.06423.x. Epub 2009 Oct 7. PMID: 19811607. 3. Aourz N, De Bundel D, Stragier B, Clinckers R, Portelli J, Michotte Y, Smolders I. Rat hippocampal somatostatin sst3 and sst4 receptors mediate anticonvulsive effects in vivo: indications of functional interactions with sst2 receptors. Neuropharmacology. 2011 Dec;61(8):1327-33. doi: 10.1016/j.neuropharm.2011.08.003. Epub 2011 Aug 16. PMID: 21854790. 4. Moneta D, Richichi C, Aliprandi M, Dournaud P, Dutar P, Billard JM, Carlo AS, Viollet C, Hannon JP, Fehlmann D, Nunn C, Hoyer D, Epelbaum J, Vezzani A. Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice. Eur J Neurosci. 2002 Sep;16(5):843-9. doi: 10.1046/j.1460-9568.2002.02146.x. PMID: 12372020.

In vitro protocol:

In vivo protocol:

1. Aourz N, De Bundel D, Stragier B, Clinckers R, Portelli J, Michotte Y, Smolders I. Rat hippocampal somatostatin sst3 and sst4 receptors mediate anticonvulsive effects in vivo: indications of functional interactions with sst2 receptors. Neuropharmacology. 2011 Dec;61(8):1327-33. doi: 10.1016/j.neuropharm.2011.08.003. Epub 2011 Aug 16. PMID: 21854790. 2. Moneta D, Richichi C, Aliprandi M, Dournaud P, Dutar P, Billard JM, Carlo AS, Viollet C, Hannon JP, Fehlmann D, Nunn C, Hoyer D, Epelbaum J, Vezzani A. Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice. Eur J Neurosci. 2002 Sep;16(5):843-9. doi: 10.1046/j.1460-9568.2002.02146.x. PMID: 12372020.