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CYN 154806 TFA

Cat. No. M10309
CYN 154806 TFA Structure
Size Price Availability Quantity
1mg USD 180  USD180 In stock
5mg USD 580  USD580 In stock
10mg USD 980  USD980 In stock
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Quality Control & Documentation
Biological Activity

CYN 154806 TFA is a cyclic octapeptide and an effective selective somatostatin sst2 receptor antagonist. 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).

Chemical Information
Molecular Weight 1311.36
Formula C58H69F3N12O16S2
CAS Number 183658-72-2 (free base)
Solubility (25°C) Water 47 mg/mL
Storage -20°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Koji Takeuchi, et al. Front Pharmacol. Activation of Muscarinic Acetylcholine Receptor Subtype 4 Is Essential for Cholinergic Stimulation of Gastric Acid Secretion: Relation to D Cell/Somatostatin

[2] W Feniuk, et al. Neuropharmacology. Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806

[3] R T Bass, et al. Mol Pharmacol. Identification and characterization of novel somatostatin antagonists

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