BIM 23052

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 . 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 . Clinical trial: Up to now, BIM-23052 is still in the preclinical development stage.

Product information

CAS Number: 133073-82-2

Molecular Weight: 1122.32

Formula: C61H75N11O10

Chemical Name: (Z,2S)-6-amino-2-[(Z)-[(2R)-2-[(Z)-[(2S)-2-[(Z)-[(2S)-2-[(Z)-[(2R)-2-amino-1-hydroxy-3-phenylpropylidene]amino]-1-hydroxy-3-phenylpropylidene]amino]-1-hydroxy-3-phenylpropylidene]amino]-1-hydroxy-3-(1H-indol-3-yl)propylidene]amino]-N-[(1S,2R)-2-hydroxy-1-[(Z)-[(1S)-1-[(Z)-[(1S,2R)-2-hydroxy-1-(C-hydroxycarbonimidoyl)propyl]-C-hydroxycarbonimidoyl]-2-phenylethyl]-C-hydroxycarbonimidoyl]propyl]hexanimidic acid

Smiles: C[C@@H](O)[C@H](/N=C(\O)/[C@H](CCCCN)/N=C(\O)/[C@@H](CC1=CNC2=CC=CC=C12)/N=C(\O)/[C@H](CC1C=CC=CC=1)/N=C(\O)/[C@H](CC1C=CC=CC=1)/N=C(\O)/[C@H](N)CC1C=CC=CC=1)/C(/O)=N/[C@@H](CC1C=CC=CC=1)/C(/O)=N/[C@@H]([C@@H](C)O)C(=N)O

InChiKey: HMTCBXPQKWFOMG-QWXJMLLVSA-N

InChi: InChI=1S/C61H75N11O10/c1-37(73)52(54(64)75)71-60(81)50(34-42-25-13-6-14-26-42)70-61(82)53(38(2)74)72-56(77)47(29-17-18-30-62)66-59(80)51(35-43-36-65-46-28-16-15-27-44(43)46)69-58(79)49(33-41-23-11-5-12-24-41)68-57(78)48(32-40-21-9-4-10-22-40)67-55(76)45(63)31-39-19-7-3-8-20-39/h3-16,19-28,36-38,45,47-53,65,73-74H,17-18,29-35,62-63H2,1-2H3,(H2,64,75)(H,66,80)(H,67,76)(H,68,78)(H,69,79)(H,70,82)(H,71,81)(H,72,77)/t37-,38-,45-,47+,48+,49+,50+,51-,52+,53+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.