Referencia número: HY-16381

Pasireotide

(Synonyms: SOM230)

6 Cited Publications

Revisión del cliente

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, pK_i=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.

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Pureza: 99.94%
No. CAS: 396091-73-9
Fòrmula: C₅₈H₆₆N₁₀O₉
Peso molecular:1047.21

Almacenamiento:

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)

Pasireotide Chemical Structure

No. CAS: 396091-73-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)^[1]

Ver todos los productos específicos de isoformas Somatostatin Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
Pituitary gland cell	IC₅₀	0.4 nM Compound: 25	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	[PMID: 12773038]
Pituitary gland cell	IC₅₀	0.4 nmol/L Compound: 25	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	[PMID: 12773038]

In Vitro

Pasireotide exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=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.

In Vivo

Pasireotide (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre^[2].
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.

Animal Model:

12 month-old conditional Men1 knockout mice with insulinoma^[2]
Dosage:

160 mg/kg/mouth
Administration:

S.c. every month for 4 months
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.

Chemical Information

No. CAS 396091-73-9
Appearance Solid
Peso molecular 1047.21
Fòrmula C₅₈H₆₆N₁₀O₉
Color White to off-white
Synonyms

SOM230
Sequence

Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-Lys-{Tyr(4-Bzl)}-Phe]
Sequence Shortening

Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-K-{Tyr(4-Bzl)}-F]
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

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.
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.
Basic Clin Pharmacol Toxicol

Somatostatin receptor ligands suppressed proliferation and lipogenesis in 3T3-L1 preadipocytes. [Abstract]

2022 Sep;131(3):174-188. PMID: 35688794
Universidad De Salamanca

2022 Oct.

Solvente y solubilidad

In Vitro:

H₂O : 45.45 mg/mL (43.40 mM; adjust pH to 1 with 1 M HCl)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9549 mL

4.7746 mL

9.5492 mL

5 mM

0.1910 mL

0.9549 mL

1.9098 mL

10 mM

0.0955 mL

0.4775 mL

0.9549 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (287 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Pasireotide

6 Cited Publications

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Pasireotide

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Cardiotoxic Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Pasireotide

Ver todos los productos específicos de isoformas Somatostatin Receptor

Actividad biológica

Chemical Information

Publications (6)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pasireotide Related Classifications

HY-16381 Related Classifications