BIM 23056

BIM 23056 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  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.

• Sicherheitsprofil

  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

• Einzelnachweise

  [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.

BIM 23056 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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