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RTI-13951-33 hydrochloride

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Catalog No. T12778
Alias RTI-13951-33 hydrochloride (2244884-08-8 free base)

RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, exhibiting an EC50 of 25 nM in vitro cAMP functional assay. It significantly reduces alcohol reinforcement and intake behaviors in rats [1].

RTI-13951-33 hydrochloride

RTI-13951-33 hydrochloride

😃Good
Catalog No. T12778Alias RTI-13951-33 hydrochloride (2244884-08-8 free base)
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, exhibiting an EC50 of 25 nM in vitro cAMP functional assay. It significantly reduces alcohol reinforcement and intake behaviors in rats [1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mgInquiry3-6 months3-6 months
50 mgInquiry3-6 months3-6 months
100 mgInquiry3-6 months3-6 months
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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
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, exhibiting an EC50 of 25 nM in vitro cAMP functional assay. It significantly reduces alcohol reinforcement and intake behaviors in rats [1].
Targets&IC50
GPR88:(EC50)25 nM
In vitro
RTI-13951-33 is a potent and selective GPR88 agonist that effectively crosses the blood-brain barrier, demonstrating a significant effect with an EC50 value of 25 nM in GPR88 cAMP functional assays. It also increases [35S]-GTPγS binding in the mouse striatum with an EC50 of 535 nM, a response absent in GPR88 knockout (KO) mice. Despite its primary activity, RTI-13951-33 exhibits weak affinities for the kappa opioid receptor (KOR; Ki, 2.29 μM), the vesicular monoamine transporter (VMAT; Ki, 4.23 μM), and a moderate affinity for the serotonin transporter (SERT; Ki, 0.75 μM). However, it demonstrates poor inhibition of SERT, with an IC50 of 25.1±2.7 μM.
In vivo
RTI-13951-33 (10 and 20 mg/kg, i.p.) reduces alcohol lever responses in a rat model of alcohol self-administration dose-dependently, demonstrating sufficient brain penetration with a half-life of 48 minutes in plasma and 87 minutes in brain [1].
SynonymsRTI-13951-33 hydrochloride (2244884-08-8 free base)
Chemical Properties
Molecular Weight532.5
FormulaC28H35Cl2N3O3
SmilesCOCC1=CC=C(C2=CC=C(N(C[C@@H](N)[C@@H](C)OC)C([C@H]3[C@H](C4=CC=CC=N4)C3)=O)C=C2)C=C1.Cl.Cl
Relative Density.no data available
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: 125 mg/mL (234.74 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.2 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 mM1.8779 mL9.3897 mL18.7793 mL93.8967 mL
5 mM0.3756 mL1.8779 mL3.7559 mL18.7793 mL
10 mM0.1878 mL0.9390 mL1.8779 mL9.3897 mL
20 mM0.0939 mL0.4695 mL0.9390 mL4.6948 mL
50 mM0.0376 mL0.1878 mL0.3756 mL1.8779 mL
100 mM0.0188 mL0.0939 mL0.1878 mL0.9390 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

Keywords

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