| BIM 23052sst5 receptor agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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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. | 133073-82-2 | SDF | Download SDF |
| Canonical SMILES | C[C@](O)([H])[C@@](/N=C(O)/[C@](/N=C(O)/[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=CC=C3)([H])CC4=CNC5=CC=CC=C45)([H])CCCCN)([H])[C@@](O)([H])C)([H])CC6=CC=CC=C6)([H])C(O)=N | ||
| Formula | C61H75N11O10 | M.Wt | 1122.3 |
| Solubility | Soluble to 1 mg/ml in sterile water | Storage | Store 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. | ||
IC90: 0.0037 nM for rat SSTR5, 3.6 nM for human SSTR5
Somatostatin receptor type 5 is a protein that in humans is encoded by the SSTR5 gene. Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. SSTR5 is a member of the superfamily of receptors having seven transmembrane segments. BIM 23052 is a linear somatostatin agonist, which displays high binding affinity for the cloned rat sst5 receptor
In vitro: BIM 23052 and the CGP 23996-like compounds bind selectively to rat SSTR5 versus human SSTR1, mouse SSTR2, mouse SSTR3, and human SSTR4.The linear compound BIM 23052 displayed approximately 1000-fold lower affinity for human SSTR5 than for rat SSTR5. Compounds that bind potently to human SSTR5, such as L-362, 855 and BIM 23052, are relatively less potent in GH inhibition [1].
In vivo: BIM 23052 (0.4, 0.8, and 1.2 nmol/rat i.c.) stimulated gastric transit; values of gastric emptying were 65.5 +/- 6.5, 77.4 +/- 5.3, and 77.7 +/- 1.9%, respectively, compared with 43.2 +/-3.2% in i.c. saline group. Intravenous injection of BIM 23052 (0.8 nmol/rat) had no effect. BIM 23052 (0.8 nmol/rat i.c.) action was prevented by subdiaphragmatic vagotomy or atropine [2].
Clinical trial: Up to now, BIM-23052 is still in the preclinical development stage.
References:[1] O"Carroll AM, Raynor K, Lolait SJ, Reisine T. Characterization of cloned human somatostatin receptor SSTR5. Mol Pharmacol. 1994 Aug;46(2):291-8.[2] Martínez V, Rivier J, Coy D, Taché Y. Intracisternal injection of somatostatin receptor 5-preferring agonists induces a vagal cholinergic stimulation of gastric emptying in rats. J Pharmacol Exp Ther. 2000 Jun;293(3):1099-105.
