BIM 23056
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Description: sst ligand
Biological Activity
Somatostatin receptor ligand (Ki values are 142, > 1000, 10.8, 16.6 and 5.7 nM for human cloned sst1 - 5 receptors respectively). Behaves as an antagonist on SRIF14-induced [35S]-GTPγS binding at sst3 and sst5 receptors (PKB values are 6.33 and 5.84 respectively).Technical Data
M.Wt:
1232.49
Formula:
C71H81N11O9
Sequence:
FFYWKVFX
(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = D-Nal & C-terminal amide)
Solubility:
Soluble to 1 mg/ml in 20% acetonitrile / water
Storage:
Desiccate at -20°C
CAS No:
150155-61-6
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
-
Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Patel and Srikant
Endocrinology, 1994;135:2814 -
Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Raynor et al.
Mol.Pharmacol., 1993;43:838 -
Characterisation of human recombinant somatostatin receptors. Modulation of GTPgammaS binding.
Siehler and Hoyer
Naunyn Schmiedebergs Arch.Pharmacol., 1999;360:500 -
Potent antagonism by BIM-23056 at the human recombinant somatostatin sst5 receptor.
Wilkinson et al.
Br.J.Pharmacol., 1996;118:445
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