CYN 154806

CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.

Product information

CAS Number: 183658-72-2

Molecular Weight: 1197.34

Formula: C56H68N12O14S2

Chemical Name: (Z,2S)-N-[(4R,7S,10S,13R,16S,19S)-10-(4-aminobutyl)-6,9,12,15,18-pentahydroxy-4-[(Z)-[(1R)-1-(C-hydroxycarbonimidoyl)-2-(4-hydroxyphenyl)ethyl]-C-hydroxycarbonimidoyl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-[(1H-indol-3-yl)methyl]-1,2-dithia-5,8,11,14,17-pentaazacycloicosa-5,8,11,14,17-pentaen-19-yl]-2-[(Z)-(1-hydroxyethylidene)amino]-3-(4-nitrophenyl)propanimidic acid

Smiles: C/C(/O)=N/[C@@H](CC1C=CC(=CC=1)N(=O)=O)/C(/O)=N/[C@@H]1CSSC[C@H](N=C(O)[C@@H](N=C(O)[C@H](CCCCN)N=C(O)[C@@H](CC2=CNC3=CC=CC=C23)N=C(O)[C@H](CC2C=CC(O)=CC=2)N=C1O)[C@@H](C)O)/C(/O)=N/[C@H](CC1C=CC(O)=CC=1)C(=N)O |c:25,29,38,54,t:67|

InChiKey: RDTVTSXTFYXNSG-HDNDNHAUSA-N

InChi: InChI=1S/C56H68N12O14S2/c1-30(69)48-56(80)66-47(54(78)62-42(49(58)73)23-33-12-18-37(71)19-13-33)29-84-83-28-46(65-51(75)43(60-31(2)70)24-32-10-16-36(17-11-32)68(81)82)55(79)63-44(25-34-14-20-38(72)21-15-34)52(76)64-45(26-35-27-59-40-8-4-3-7-39(35)40)53(77)61-41(50(74)67-48)9-5-6-22-57/h3-4,7-8,10-21,27,30,41-48,59,69,71-72H,5-6,9,22-26,28-29,57H2,1-2H3,(H2,58,73)(H,60,70)(H,61,77)(H,62,78)(H,63,79)(H,64,76)(H,65,75)(H,66,80)(H,67,74)/t30-,41+,42-,43+,44+,45-,46-,47+,48+/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

How to use

In Vitro:

CYN 154806 inhibits SRIF-induced increases in extracellular acidification (EAR) in CHO-K1 cells expressing human sst2 receptors (pKB 7.92). CYN 154806 also blocks SRIF-induced increases [35S]-GTPγS binding in CHO-K1 cell membranes expressing human sst2 receptors as well as rat sst2(a) and rat sst2(b) receptors (pKB 7.81, 7.68 and 7.96, respectively).

In Vivo:

CYN 154806 (0.1 mg/kg; i.p.; 20 min before the administration of carbachol (CCh) (30 μg/kg) in M4 KO mice) dose-dependently and significantly reverses the decreases acid response to CCh in M4 but not M3 KO mice.

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