BIM 23056

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。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
1mg

￥2725.00

2180.00

- +
5mg

￥8100.00

6480.00

- +
10mg

￥12825.00

10260.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci17042
CAS: 150155-61-6
别名:
分子式: C71H81N11O9
分子量: 1232.49
纯度: >98%
溶解度: Soluble to 1 mg/ml in 20% acetonitrile / Water
储存: Desiccate at -20°C
库存: 现货

Background

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.

参考文献:
[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.