2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. RLX-33

RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome.

For research use only. We do not sell to patients.

RLX-33 Chemical Structure

RLX-33 Chemical Structure

CAS No. : 2784577-71-3

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5 mg USD 380 In-stock
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Based on 1 publication(s) in Google Scholar

RLX-33 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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Description

RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome[1].

IC50 & Target

IC50: 2.36 μM (RXFP3), 7.82 μM (ERK1 phosphorylation), 13.86 μM (ERK2 phosphorylation)[1]
In Vivo

RLX-33 (10 mg/kg; IP, single dosage) attenuates the RXFP3-selective agonist R3/I5-induced increase in feeding in male Wistar rats[1].
RLX-33 (10 mg/kg; IP, single dosage) exhibits a good brain penetration and highly protein-bound in rats plasma[1].
Pharmacokinetic Parameters of RLX-33 in male Wistar rats (IP, 10 mg/kg)[1].

plasma brain
Cmax (ng/mL) 1401 1552
tmax (h) 0.5 2.0
t1/2 (h) 1.9 4.9
AUCinf (ng/mL·h) 5352 12519
CL_F (mL/min/kg) 43.8

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake[1]
Dosage: 10 mg/kg
Administration: IP, single dosage
Result: Attenuated the R3/I5-induced increase in food intake.
Animal Model: Male Wistar rats[1]
Dosage: 10 mg/kg
Administration: IP, single dosage (Pharmacokinetic Analysis)
Result: Exhibited a good brain penetration and highly protein-bound, with protein binding of 99.8% in rat plasma.
Molecular Weight

462.89

Formula

C24H19ClN4O4
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C(C1)CN(CC2=CC=CO2)C1=O)NC3=CC=C(C4=NC(C5=CC=C(Cl)C=C5)=NO4)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (270.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1603 mL 10.8017 mL 21.6034 mL
5 mM 0.4321 mL 2.1603 mL 4.3207 mL
View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1603 mL 10.8017 mL 21.6034 mL 54.0085 mL
5 mM 0.4321 mL 2.1603 mL 4.3207 mL 10.8017 mL
10 mM 0.2160 mL 1.0802 mL 2.1603 mL 5.4009 mL
15 mM 0.1440 mL 0.7201 mL 1.4402 mL 3.6006 mL
20 mM 0.1080 mL 0.5401 mL 1.0802 mL 2.7004 mL
25 mM 0.0864 mL 0.4321 mL 0.8641 mL 2.1603 mL
30 mM 0.0720 mL 0.3601 mL 0.7201 mL 1.8003 mL
40 mM 0.0540 mL 0.2700 mL 0.5401 mL 1.3502 mL
50 mM 0.0432 mL 0.2160 mL 0.4321 mL 1.0802 mL
60 mM 0.0360 mL 0.1800 mL 0.3601 mL 0.9001 mL
80 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6751 mL
100 mM 0.0216 mL 0.1080 mL 0.2160 mL 0.5401 mL
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RLX-33 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RLX-332784577-71-3RLX33RLX 33ERKExtracellular signal regulated kinasesBBBrelaxinRXFP3metabolic syndromeWistar ratsR3/I5Inhibitorinhibitorinhibit

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