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BIM 23056
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BIM 23056图片
CAS NO:150155-61-6
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
BIM 23056 是一种线性八肽，是一种有效的 sst3 和 sst5 生长抑素受体拮抗剂，Ki 值分别为 10.8 和 5.7。
Cas No.150155-61-6
Canonical SMILESCC([C@@](/N=C(O)/[C@](/N=C(O)/[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@@](N)([H])CC1=CC=CC=C1)([H])CC2=CC=CC=C2)([H])CC3=CC=C(O)C=C3)([H])CC4=CNC5=CC=CC=C45)([H])CCCCN)([H])/C(O)=N/[C@@](/C(O)=N/[C@](C(O)=N)([H])CC6=CC7=CC=CC=C7C=C6)([H])CC8=CC=CC=C8)C
分子式C71H81N11O9
分子量1232.49
溶解度Soluble to 1 mg/ml in 20% acetonitrile / Water
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 0.02 nM for SSTR3

Somatostatin (SRIF) is a cyclic tetradecapeptide that was originally isolated from mammalian hypothalamus and characterized as a physiological regulator of GH secretion from the anterior pituitary. BIM 23056 is a novel linear peptide of SRIF SSTR3 antagnist.

In vitro: BIM 23056 bound to SSTR3 with subnanomolar affinities. BIM 23056 displayed remarkable selectivity for SSTR3, not interacting significantly with either SSTR1 or SSTR2 at concentrations as high as 1 μM. BIM 23056 was 30,000-fold selective for SSTR3, which maks it a ligand of choice for future studies on SSTR3 [1]. In addition, it has been found that BIM 23056 behaves as a potent and surmountable antagonist at the human recombinant sst5 receptor. Such antagonism was specific for the sst5 receptor as BIM 23056 did not inhibit [Ca2+], or Ins(1,4,5)P3 increases in response to UTP [2].

In vivo: No animal in vivo data have been reported.

Clinical trial: Up to now, BIM 23056 is still in the preclinical development stage.

References:
[1] Raynor K, Murphy WA, Coy DH, Taylor JE, Moreau JP, Yasuda K, Bell GI, Reisine T.  Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. Mol Pharmacol. 1993 Jun;43(6):838-44.
[2] Wilkinson GF, Thurlow RJ, Sellers LA, Coote JE, Feniuk W, Humphrey PP.  Potent antagonism by BIM-23056 at the human recombinant somatostatin sst5 receptor. Br J Pharmacol. 1996 Jun;118(3):445-7.