Pasireotide (aspartate) (trifluoroacetate salt)
(Synonyms: SOM230) 目录号 : GC47925
A somatostatin receptor agonist
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pasireotide is a somatostatin receptor (SSTR) agonist that binds selectively to SST1, SST2, SST3, and SST5 over SST4 (IC50s = 9.3, 1, 1.5, 0.16, and >100 nM, respectively, for human recombinant receptors).1 It dose-dependently inhibits growth hormone release stimulated by growth hormone-releasing hormone (GHRH) in primary rat anterior pituitary cells and inhibits adrenocorticotropic hormone (ACTH) secretion by some primary human corticotrope adenomas at a concentration of 10 nM.1,2 Pasireotide (10 nM) also inhibits ACTH release from and proliferation of mouse AtT20 pituitary corticotrope cells in vitro and inhibits tumor growth of subcutaneously implanted AtT20 cells in vivo in nude mice when administered at a dose of 1.5 μg per day.3 Pasireotide (0.03 mg/kg) decreases plasma ACTH concentrations and tumor size in dogs with ACTH-dependent Cushing's disease.4 Formulations containing pasireotide have been used in the treatment of acromegaly and Cushing's disease.
1.Bruns, C., Lewis, I., Briner, U., et al.SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profileEur. J. Endocrinol.146(5)707-716(2002) 2.Hofland, L.J., van der Hoek, J., Feelders, R., et al.The multi-ligand somatostatin analogue SOM230 inhibits ACTH secretion by cultured human corticotroph adenomas via somatostatin receptor type 5Eur. J. Endocrinol.152(4)645-654(2005) 3.Murasawa, S., Kageyama, K., Sugiyama, A., et al.Inhibitory effects of SOM230 on adrenocorticotropic hormone production and corticotroph tumor cell proliferation in vitro and in vivoMol. Cell. Endocrinol.394(1-2)37-46(2014) 4.Castillo, V., Theodoropoulou, M., Stalla, J., et al.Effect of SOM230 (pasireotide) on corticotropic cells: Action in dogs with Cushing's diseaseNeuroendocrinology94(2)124-136(2011)
| Cas No. | N/A | SDF | |
| 别名 | SOM230 | ||
| Canonical SMILES | O=C([C@H](CC1=CC=CC=C1)N2)N3[C@](C[C@@H](OC(NCCN)=O)C3)([H])C(N[C@H](C4=CC=CC=C4)C(N[C@H](CC5=CNC6=C5C=CC=C6)C(N[C@@H](CCCCN)C(N[C@@H](CC7=CC=C(OCC8=CC=CC=C8)C=C7)C2=O)=O)=O)=O)=O.OC(C[C@H](N)C(O)=O)=O.OC(C[C@H](N)C(O)=O)=O.FC(F)(C(O)=O)F | ||
| 分子式 | C58H66N10O9.2C4H7NO4.XCF3COOH | 分子量 | 1313.4 |
| 溶解度 | DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 33 mg/ml,Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml | 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 | 0.7614 mL | 3.8069 mL | 7.6138 mL |
| 5 mM | 0.1523 mL | 0.7614 mL | 1.5228 mL |
| 10 mM | 0.0761 mL | 0.3807 mL | 0.7614 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。