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

RLX-33 

Cat. No.: HY-150700 Purity: 99.79%
COA Handling Instructions

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
10 mg USD 600 In-stock
25 mg USD 1150 In-stock
50 mg USD 1800 In-stock
100 mg USD 2850 In-stock
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Based on 1 publication(s) in Google Scholar

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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

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

Appearance

Solid

Formula

C24H19ClN4O4

CAS No.
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)

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
10 mM 0.2160 mL 1.0802 mL 2.1603 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Product Name:
RLX-33
Cat. No.:
HY-150700
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