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Pasireotide pamoate

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Catalog No. T12369Cas No. 396091-79-5
Alias SOM230 pamoate

Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

Pasireotide pamoate

Pasireotide pamoate

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Catalog No. T12369Alias SOM230 pamoateCas No. 396091-79-5
Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
Targets&IC50
SST2:9 (pki), SST5:9.9(pki), SST1:pki:8.2 , SST4:<7.0 (pki), SST3:9.1(pki)
In vitro
SOM230, a novel, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1-sst5).?SOM230 has potent, long-lasting inhibitory effects on growth hormone and insulin-like growth factor-1 release[1]
In vivo
Untreated SSTR2(-/-) mice with AIA displayed joint swelling and mechanical hyperalgesia similar to that seen in SSTR2(+/+) mice.?In wild-type mice, both octreotide and pasireotide significantly attenuated knee joint swelling and histopathologic manifestations of arthritis to an extent comparable to that of dexamethasone.?In SSTR2(-/-) mice, the antiinflammatory effects of both octreotide and pasireotide were completely abrogated.?Prolonged administration of pasireotide also inhibited joint swelling and protected against joint destruction during AIA flare reactions.?In addition, both octreotide and pasireotide reduced inflammatory hyperalgesia.?The antinociceptive actions of octreotide were abolished in SSTR2(-/-) mice, but those of pasireotide were retained.?In dorsal root ganglia of naive wild-type mice, only SSTR1 and SSTR2A, but not SSTR3 or SSTR5, were detected in a subset of small- and medium-diameter neurons[1].
SynonymsSOM230 pamoate
Chemical Properties
Molecular Weight1435.58
FormulaC81H82N10O15
Cas No.396091-79-5
SmilesC(C=1C2=C(C=C(C(O)=O)C1O)C=CC=C2)C=3C4=C(C=C(C(O)=O)C3O)C=CC=C4.O=C1N2[C@@](C[C@@H](OC(NCCN)=O)C2)(C(=O)N[C@](C(=O)N[C@H](CC=3C=4C(NC3)=CC=CC4)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CC=C(OCC6=CC=CC=C6)C=C5)C(=O)N[C@H]1CC7=CC=CC=C7)(C8=CC=CC=C8)[H])[H]
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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