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RLX-33

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Catalog No. T62929Cas No. 2784577-71-3

RLX-33 is a potent and selective antagonist of relaxin family peptide 3 (RXFP3) that crosses the blood-brain barrier and also blocks relaxin 3-induced ERK1/2 phosphorylation. RLX-33 can block the increase in food intake induced by the RXFP3 selective agonist R3/I5 in rats.RLX-33 can be used to study the metabolic syndrome.

RLX-33

RLX-33

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Purity: 99.89%
Catalog No. T62929Cas No. 2784577-71-3
RLX-33 is a potent and selective antagonist of relaxin family peptide 3 (RXFP3) that crosses the blood-brain barrier and also blocks relaxin 3-induced ERK1/2 phosphorylation. RLX-33 can block the increase in food intake induced by the RXFP3 selective agonist R3/I5 in rats.RLX-33 can be used to study the metabolic syndrome.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$75In StockIn Stock
5 mg$187In StockIn Stock
10 mg$298In StockIn Stock
25 mg$475In StockIn Stock
50 mg$678In StockIn Stock
100 mg$912In StockIn Stock
500 mg$1,780-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.89%
Appearance:Solid
Color:White
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Product Introduction

RLX-33 AI Summary
RLX-33 is a multi-target agent with diverse bioactivities. It exhibits an efflux ratio of 1.0 in MDCK-MDR1 cells and shows antagonist activity at human RXFP3 with IC50 values of 3080.0 nM and 4520.0 nM, while its activity as an antagonist at human RXFP4 is below 30.0%. The compound has different pharmacokinetic parameters in Wistar rat plasma and brain, including Cmax, Tmax, AUC, half-life, and unbound clearance. It demonstrates a Papp value of 1.3 x 10^-6 cm/s across the apical to basolateral sides in MDCK-MDR1 cells and exhibits low kinetic aqueous solubility (< 1000.0 nM). Additionally, it has high plasma protein binding at 99.8% in Wistar rats. RLX-33 also inhibits a range of receptors, including sigma-2, sigma-1, 5HT2C, muscarinic, opioid, serotonin, adrenergic, DAT, NET, SERT, GABAA, histamine, and PBR receptors, with inhibition levels below 50%..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
RLX-33 is a potent and selective antagonist of relaxin family peptide 3 (RXFP3) that crosses the blood-brain barrier and also blocks relaxin 3-induced ERK1/2 phosphorylation. RLX-33 can block the increase in food intake induced by the RXFP3 selective agonist R3/I5 in rats.RLX-33 can be used to study the metabolic syndrome.
Targets&IC50
RXFP3:2.36 μM
Chemical Properties
Molecular Weight462.89
FormulaC24H19ClN4O4
Cas No.2784577-71-3
SmilesN(C(=O)C1CN(CC2=CC=CO2)C(=O)C1)C3=CC=C(C4=NC(=NO4)C5=CC=C(Cl)C=C5)C=C3
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: 112.5 mg/mL (243.04 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 3.3 mg/mL (7.13 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 mM2.1603 mL10.8017 mL21.6034 mL108.0170 mL
5 mM0.4321 mL2.1603 mL4.3207 mL21.6034 mL
10 mM0.2160 mL1.0802 mL2.1603 mL10.8017 mL
20 mM0.1080 mL0.5401 mL1.0802 mL5.4009 mL
50 mM0.0432 mL0.2160 mL0.4321 mL2.1603 mL
100 mM0.0216 mL0.1080 mL0.2160 mL1.0802 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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