BIM 23056Somatostatin receptor ligand |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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Cas No. | 150155-61-6 | SDF | Download SDF |
Canonical SMILES | CC([C@@](/N=C(O)/[C@](/N=C(O)/[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@@](N)([H])CC1=CC=CC=C1)([H])CC2=CC=CC=C2)([H])CC3=CC=C(O)C=C3)([H])CC4=CNC5=CC=CC=C45)([H])CCCCN)([H])/C(O)=N/[C@@](/C(O)=N/[C@](C(O)=N)([H])CC6=CC7=CC=CC=C7C=C6)([H])CC8=CC=CC=C8)C | ||
Formula | C71H81N11O9 | M.Wt | 1232.49 |
Solubility | Soluble to 1 mg/ml in 20% acetonitrile / H2O | Storage | Desiccate at -20°C |
Physical Appearance | White lyophilised solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
IC50: 0.02 nM for SSTR3
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.
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].
In vivo: No animal in vivo data have been reported.
Clinical trial: Up to now, BIM 23056 is still in the preclinical development stage.
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.