| Identification | Back 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 | [MDL Number]
MFCD00929082 | [MOL File]
150155-61-6.mol | [Molecular Weight]
1232.47 |
| Chemical Properties | Back 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
| [Water Solubility ]
H2O: >1mg/mL |
| Safety Data | Back Directory | [WGK Germany ]
3
| [Storage Class]
11 - Combustible Solids | [Toxicity]
TDLo ice-rat: 45.415 mg/kg JPETAB 293,1099,2000 |
| Hazard Information | Back Directory | [Uses]
BIM 23056, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with Ki values of 10.8, 5.7, respectively[1]. | [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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BOC Sciences
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| Website: |
https://www.bocsci.com |
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