CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC 50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
性状
Solid
IC50 & Target[1][2]
SSTR2
体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
CYN 154806 TFA (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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
[1]. Bass RT, et al. Identification and characterization of novel somatostatin antagonists. Mol Pharmacol. 1996 Oct;50(4):709-15.[2]. Feniuk W, et al. Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology. 2000 Jun 8;39(8):1443-50.[3]. Takeuchi K, et al. A
溶解度数据
In Vitro: H2O : 25 mg/mL (19.06 mM; Need ultrasonic)配制储备液