Pasireotide
Based on 6 publication(s) in Google Scholar
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 396091-73-9
- 分子式: C58H66N10O9
- 分子量:1047.21
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Pasireotide
More- Hepatology. 2017 Oct;66(4):1197-1218. [Abstract]
- J Clin Invest. 2024 Aug 13;134(19):e178604. [Abstract]
- Commun Med (Lond). 2022 Jul 1:2:80. [Abstract]
- Am J Pathol. 2018 Apr;188(4):981-994. [Abstract]
- Basic Clin Pharmacol Toxicol. 2022 Sep;131(3):174-188. [Abstract]
- Universidad De Salamanca. 2022 Oct.
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
生物活性
pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Pituitary gland cell | IC50 |
0.4 nM
Compound: 25
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In vitro inhibition of GHRH induced GH release in primary cultures of rat pituitary cells
In vitro inhibition of GHRH induced GH release in primary cultures of rat pituitary cells
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[PMID: 12773038] |
| Pituitary gland cell | IC50 |
0.4 nmol/L
Compound: 25
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In vitro inhibition of GHRH induced GH release in primary cultures of rat pituitary cells
In vitro inhibition of GHRH induced GH release in primary cultures of rat pituitary cells
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[PMID: 12773038] |
Pasireotide exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively)[1].
Pasireotide effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC50 of 0.4 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pasireotide (2-50 μg/kg; s.c. twice daily for 42 days) exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:12 month-old conditional Men1 knockout mice with insulinoma[2]
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Dosage:160 mg/kg/mouth
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Administration:S.c. every month for 4 months
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Result:Decreased the serum insulin from 1.060 μg/L to 0.3653 μg/L and increased the serum glucose from 4.246 mM to 7.122 mM.
Significantly reduced the tumor size and increased apoptosis.
化学情報
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CAS 番号 396091-73-9
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性状 Solid
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分子量 1047.21
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分子式 C58H66N10O9
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Color White to off-white
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別名
SOM230
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配列
Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-Lys-{Tyr(4-Bzl)}-Phe]
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シーケンスの短縮
Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-K-{Tyr(4-Bzl)}-F]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Hepatology
TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. [Abstract]2017 Oct;66(4):1197-1218. PMID: 28543567
Pasireotide purchased from MedChemExpress. Usage Cited in: Hepatology. 2017 Oct;66(4):1197-1218. [Abstract]
Concurrent treatment of ADPKD cholangiocytes by SBI-115 and Pasireotide decreases cell proliferation, cholangiocyte spheroid growth, and cAMP levels.
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J Clin Invest
Genomic and transcriptomic features of androgen receptor signaling inhibitor resistance in metastatic castration-resistant prostate cancer. [Abstract]2024 Aug 13;134(19):e178604. PMID: 39352383 -
Commun Med (Lond)
Patient-derived tumor organoids for personalized medicine in a patient with rare hepatocellular carcinoma with neuroendocrine differentiation: a case report. [Abstract]2022 Jul 1:2:80. PMID: 35789568 -
Am J Pathol
Combination of a Histone Deacetylase 6 Inhibitor and a Somatostatin Receptor Agonist Synergistically Reduces Hepatorenal Cystogenesis in an Animal Model of Polycystic Liver Disease. [Abstract]2018 Apr;188(4):981-994. PMID: 29366679
Pasireotide purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2018 Apr;188(4):981-994. [Abstract]
Representative western blot and quantitation of band density show an increase expression of acetylated α-tubulin in PCK cholangiocytes upon ACY-1215 and ACY-1215+Pasireotide treatment.
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Basic Clin Pharmacol Toxicol
Somatostatin receptor ligands suppressed proliferation and lipogenesis in 3T3-L1 preadipocytes. [Abstract]2022 Sep;131(3):174-188. PMID: 35688794 -
溶剤 & 溶解度
H2O : 45.45 mg/mL (43.40 mM; adjust pH to 1 with 1 M HCl)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[1]. Lewis I, et, al. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem. 2003 Jun 5;46(12):2334-44. [Content Brief]
[2]. Quinn TJ, et, al. Pasireotide (SOM230) is effective for the treatment of pancreatic neuroendocrine tumors (PNETs) in a multiple endocrine neoplasia type 1 (MEN1) conditional knockout mouse model. Surgery. 2012 Dec;152(6):1068-77. [Content Brief]
[3]. Schmid HA, et, al. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol Cell Endocrinol. 2008 May 14;286(1-2):69-74. [Content Brief]
[4]. Imhof AK, et, al. Differential antiinflammatory and antinociceptive effects of the somatostatin analogs octreotide and pasireotide in a mouse model of immune-mediated arthritis. Arthritis Rheum. 2011 Aug;63(8):2352-62. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.9549 mL | 4.7746 mL | 9.5492 mL | 23.8730 mL |
| 5 mM | 0.1910 mL | 0.9549 mL | 1.9098 mL | 4.7746 mL | |
| 10 mM | 0.0955 mL | 0.4775 mL | 0.9549 mL | 2.3873 mL | |
| 15 mM | 0.0637 mL | 0.3183 mL | 0.6366 mL | 1.5915 mL | |
| 20 mM | 0.0477 mL | 0.2387 mL | 0.4775 mL | 1.1936 mL | |
| 25 mM | 0.0382 mL | 0.1910 mL | 0.3820 mL | 0.9549 mL | |
| 30 mM | 0.0318 mL | 0.1592 mL | 0.3183 mL | 0.7958 mL | |
| 40 mM | 0.0239 mL | 0.1194 mL | 0.2387 mL | 0.5968 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Pasireotide 関連分類
HY-16381 関連分類
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