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150155-61-6

150155-61-6 Structure

150155-61-6 Structure
IdentificationBack Directory
[Name]

BIM 23056
[CAS]

150155-61-6
[Synonyms]

BIM 23056
M.W. 1232.49 C71H81N11O9
D-PHE-PHE-TYR-D-TRP-LYS-VAL-PHE-D-NAL-NH2
D-Phe-Phe-Tyr-D-Trp-Lys-VaL-Phe-D-Nal-NH2 trifluoroacetate salt
D-Alaninamide, D-phenylalanyl-L-phenylalanyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-phenylalanyl-3-(2-naphthalenyl)-
[Molecular Formula]

C71H81N11O9
[MOL File]

150155-61-6.mol
[Molecular Weight]

1232.47
Chemical PropertiesBack Directory
[Boiling point ]

1544.6±65.0 °C(Predicted)
[density ]

1.271±0.06 g/cm3(Predicted)
[storage temp. ]

−20°C
[solubility ]

H2O: >1mg/mL
[form ]

solid
[pka]

9.82±0.15(Predicted)
[color ]

white
Safety DataBack Directory
[WGK Germany ]

3
[Toxicity]

TDLo ice-rat: 45.415 mg/kg JPETAB 293,1099,2000
Hazard InformationBack Directory
[Biological Activity]

somatostatin (srif) is a cyclic tetradecapeptide that was originally isolated from mammalian hypothalamus and characterized as a physiological regulator of gh secretion from the anterior pituitary. bim 23056 is a novel linear peptide of srif sstr3 antagnist.
[Safety Profile]

A poison by intracerebral route. When heated to decomposition it emits toxic vapors of NOx.
[in vitro]

bim 23056 bound to sstr3 with subnanomolar affinities. bim 23056 displayed remarkable selectivity for sstr3, not interacting significantly with either sstr1 or sstr2 at concentrations as high as 1 μm. bim 23056 was 30,000-fold selective for sstr3, which maks it a ligand of choice for future studies on sstr3 [1]. in addition, it has been found that bim 23056 behaves as a potent and surmountable antagonist at the human recombinant sst5 receptor. such antagonism was specific for the sst5 receptor as bim 23056 did not inhibit [ca2+], or ins(1,4,5)p3 increases in response to utp [2].
[IC 50]

0.02 nm for sstr3
[References]

[1] raynor k, murphy wa, coy dh, taylor je, moreau jp, yasuda k, bell gi, reisine t. cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. mol pharmacol. 1993 jun;43(6):838-44.
[2] wilkinson gf, thurlow rj, sellers la, coote je, feniuk w, humphrey pp. potent antagonism by bim-23056 at the human recombinant somatostatin sst5 receptor. br j pharmacol. 1996 jun;118(3):445-7.
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