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BIM 23052 Sale

目录号 : GC14119

sst5 receptor agonist

BIM 23052 Chemical Structure

Cas No.:133073-82-2

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1mg
¥1,481.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 133073-82-2 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
分子式 C61H75N11O10 分子量 1122.3
溶解度 Soluble to 1 mg/ml in sterile water 储存条件 Store at -20°C
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1 mM 0.891 mL 4.4551 mL 8.9103 mL
5 mM 0.1782 mL 0.891 mL 1.7821 mL
10 mM 0.0891 mL 0.4455 mL 0.891 mL
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