CYN 154806 TFA( —— )

Catalog No. M37914 CAS No. 2828432-46-6

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Datasheet

HNMR

HPLC

MSDS

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Product Name

CYN 154806 TFA
Note

Research use only, not for human use.
Brief Description

CYN 154806 TFA is a cyclic octapeptide and an effective selective somatostatin sst2 receptor antagonist. For the recombinant sst2, sst1, sst3, sst4 and sst5 receptors, the pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48, respectively.
Description

CYN 154806 TFA, 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.
In Vitro

CYN 154806 TFA inhibits SRIF-induced increases in extracellular acidification (EAR) in CHO-K1 cells expressing human sst2 receptors (pKB 7.92). CYN 154806 TFA 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 TFA (0.1 mg/kg; i.p.; 20 minbefore 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.
Synonyms

——
Pathway

GPCR/G Protein
Target

Somatostatin Receptor
Recptor

Somatostatin
Research Area

——
Indication

——

CAS Number

2828432-46-6
Formula Weight

1311.36
Molecular Formula

C58H69F3N12O16S2
Purity

>98% (HPLC)
Solubility

In Vitro:?H2O : 25 mg/mL (19.06 mM; Ultrasonic)
SMILES

C[C@@H](O)[C@H]1C(N[C@H](C(N[C@@H](C(N)=O)CC2=CC=C(O)C=C2)=O)CSSC[C@@H](NC([C@@H](NC(C)=O)CC3=CC=C([N+]([O-])=O)C=C3)=O)C(N[C@@H](CC4=CC=C(O)C=C4)C(N[C@H](CC5=CNC6=CC=CC=C65)C(N[C@@H](CCCCN)C(N1)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O
Chemical Name

——

1. Bass RT, et al. Identification and characterization of novel somatostatin antagonists. Mol Pharmacol. 1996 Oct;50(4):709-15.?

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