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Paltusotine

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Catalog No. T9692Cas No. 2172870-89-0

Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients

Paltusotine

Paltusotine

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Purity: 99.91%
Catalog No. T9692Cas No. 2172870-89-0
Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$178In StockIn Stock
5 mg$446In StockIn Stock
10 mg$645In StockIn Stock
25 mg$977In StockIn Stock
50 mg$1,320-In Stock
100 mg$1,780InquiryInquiry
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.91%
Appearance:Solid
Color:White
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Product Introduction

Paltusotine AI Summary
Paltusotine exhibits potent agonist activity at the human SST2 receptor with an EC50 of 0.25 nM. It also shows strong agonist activity at the rat SST2 receptor (EC50 = 1.2 nM) and dog SST2 receptor (EC50 = 6.6 nM). This compound is highly selective for the SST2 receptor over other subtypes (SST1, SST3, SST4, and SST5) with selectivity ratios greater than 1000. It inhibits human CYP2C9 and CYP2C19 enzymes with IC50 values of 7943.28 nM and 5011.87 nM, respectively. Furthermore, Paltusotine demonstrates long half-lives in human and rat liver microsomes and in Sprague-Dawley rats, along with moderate oral bioavailability in rats and dogs. Importantly, it shows low to no inhibition of hERG and human CYP2D6 and CYP3A4 enzymes..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients
Chemical Properties
Molecular Weight456.49
FormulaC27H22F2N4O
Cas No.2172870-89-0
SmilesNC1CCN(CC1)c1c(cnc2ccc(cc12)-c1cccc(C#N)c1O)-c1cc(F)cc(F)c1
Relative Density.1.41 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 20 mg/mL (43.81 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.38 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1906 mL10.9531 mL21.9063 mL109.5314 mL
5 mM0.4381 mL2.1906 mL4.3813 mL21.9063 mL
10 mM0.2191 mL1.0953 mL2.1906 mL10.9531 mL
20 mM0.1095 mL0.5477 mL1.0953 mL5.4766 mL

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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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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