BIM 23052
目录号 : GC14119
sst5 receptor agonist
Cas No.:133073-82-2
Sample solution is provided at 25 µL, 10mM.
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IC90: 0.0037 nM for rat SSTR5, 3.6 nM for human SSTR5
Somatostatin receptor type 5 is a protein that in humans is encoded by the SSTR5 gene. Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. SSTR5 is a member of the superfamily of receptors having seven transmembrane segments. BIM 23052 is a linear somatostatin agonist, which displays high binding affinity for the cloned rat sst5 receptor
In vitro: BIM 23052 and the CGP 23996-like compounds bind selectively to rat SSTR5 versus human SSTR1, mouse SSTR2, mouse SSTR3, and human SSTR4.The linear compound BIM 23052 displayed approximately 1000-fold lower affinity for human SSTR5 than for rat SSTR5. Compounds that bind potently to human SSTR5, such as L-362, 855 and BIM 23052, are relatively less potent in GH inhibition [1].
In vivo: BIM 23052 (0.4, 0.8, and 1.2 nmol/rat i.c.) stimulated gastric transit; values of gastric emptying were 65.5 +/- 6.5, 77.4 +/- 5.3, and 77.7 +/- 1.9%, respectively, compared with 43.2 +/-3.2% in i.c. saline group. Intravenous injection of BIM 23052 (0.8 nmol/rat) had no effect. BIM 23052 (0.8 nmol/rat i.c.) action was prevented by subdiaphragmatic vagotomy or atropine [2].
Clinical trial: Up to now, BIM-23052 is still in the preclinical development stage.
References:
[1] O'Carroll AM, Raynor K, Lolait SJ, Reisine T. Characterization of cloned human somatostatin receptor SSTR5. Mol Pharmacol. 1994 Aug;46(2):291-8.
[2] Martínez V, Rivier J, Coy D, Taché Y. Intracisternal injection of somatostatin receptor 5-preferring agonists induces a vagal cholinergic stimulation of gastric emptying in rats. J Pharmacol Exp Ther. 2000 Jun;293(3):1099-105.
| Cas No. | 133073-82-2 | SDF | |
| Canonical SMILES | C[C@](O)([H])[C@@](/N=C(O)/[C@](/N=C(O)/[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=CC=C3)([H])CC4=CNC5=CC=CC=C45)([H])CCCCN)([H])[C@@](O)([H])C)([H])CC6=CC=CC=C6)([H])C(O)=N | ||
| 分子式 | C61H75N11O10 | 分子量 | 1122.3 |
| 溶解度 | Soluble to 1 mg/ml in sterile water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.891 mL | 4.4551 mL | 8.9103 mL |
| 5 mM | 0.1782 mL | 0.891 mL | 1.7821 mL |
| 10 mM | 0.0891 mL | 0.4455 mL | 0.891 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet