| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
RLX-33 targets the relaxin family peptide 3 receptor (RXFP3), a G protein-coupled receptor that mediates the effects of the neuropeptide relaxin-3. By blocking RXFP3, RLX-33 prevents relaxin-3-induced signaling, including the downstream phosphorylation of ERK1 and ERK2. The compound's ability to cross the blood-brain barrier makes it valuable for studying the role of the relaxin-3/RXFP3 system in the central nervous system.
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| ln Vitro |
In vitro, RLX-33 is a potent antagonist of RXFP3 with an IC50 of 2.36 µM. It also blocks relaxin-3-induced ERK1/2 phosphorylation with IC50 values of 7.82 µM and 13.86 µM for ERK1 and ERK2, respectively. These data demonstrate its activity in blocking RXFP3-mediated signaling pathways.
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| ln Vivo |
RLX-33 (10 mg/kg; IP, single dose) attenuates the increase in food intake elicited by the RXFP3 selective agonist R3/I5 in male Wistar rats [1]. RLX-33 (10 mg/kg; IP, single dose) displays strong brain penetration and high protein binding in rat plasma [1]. Pharmacokinetic characteristics of RLX-33 in male Wistar rats (IP, 10 mg/kg) [1]. Brain plasma 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
In vivo, RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. This demonstrates its functional activity in vivo and supports its potential for research into metabolic syndrome and feeding behavior. The compound's BBB penetrance enables central nervous system activity. |
| Enzyme Assay |
A cell-free assay for RLX-33 would involve measuring its binding affinity to RXFP3 using radioligand binding assays with membrane preparations expressing the receptor. The compound's ability to displace a labeled RXFP3 ligand would be measured. Alternatively, its inhibition of ERK1/2 phosphorylation could be assessed in cell-free kinase assays. Specific protocols are not detailed.
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| Cell Assay |
Cellular assays for RLX-33 would typically involve measuring its effects on RXFP3-mediated signaling. Cells expressing RXFP3 are stimulated with relaxin-3, and ERK1/2 phosphorylation is measured. RLX-33 is added at varying concentrations to determine its IC50 for inhibiting ERK1/2 phosphorylation. These assays confirm the compound's activity in blocking RXFP3 signaling.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (Intracerebroventricular injection of R3/I5 stimulates food intake [1]
Doses: 10 mg/kg Route of Administration: IP, single dose Experimental Results: attenuates R3/I5-induced increase in food intake Animal/Disease Models: Male Wistar rat [1] Doses: 10 mg/kg Doses: IP, single dose (pharmacokinetic/PK/PK analysis) Experimental Results: It demonstrated good brain penetration and high protein binding, and the protein binding rate in rat plasma was 99.8%. In vivo animal experiments with RLX-33 have been conducted in rats. The compound blocks the stimulation of food intake induced by the RXFP3-selective agonist R3/I5. Specific dosing regimens and detailed protocols are not provided in the available sources. |
| ADME/Pharmacokinetics |
RLX-33 has a molecular formula of C24H19ClN4O4 and a molecular weight of 462.89. It is a solid powder. Specific pharmacokinetic parameters, such as half-life and bioavailability, are not provided in the available sources. The compound is BBB penetrant. For storage, the powder should be kept at -20°C for up to 3 years or at 4°C for up to 2 years.
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| Toxicity/Toxicokinetics |
Toxicity data for RLX-33 are not provided in the available sources. As a research compound, it is intended for research use only and not for human consumption. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
RLX-33 (CAS: 2784577-71-3) is a potent and selective RXFP3 antagonist with an IC50 of 2.36 µM. It also blocks relaxin-3-induced ERK1/2 phosphorylation with IC50 values of 7.82 µM and 13.86 µM for ERK1 and ERK2, respectively. The compound is BBB penetrant and can block food intake stimulation induced by RXFP3 agonists in rats. Its molecular formula is C24H19ClN4O4 and its molecular weight is 462.89. It is not an approved drug and is strictly for research purposes.
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| Molecular Formula |
C24H19CLN4O4
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| Molecular Weight |
462.88506436348
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| Exact Mass |
462.109
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| CAS # |
2784577-71-3
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| PubChem CID |
164886639
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| Appearance |
White to light yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
696
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(CC2=CC=CO2)C(=O)CC(C(NC2=CC=C(C3ON=C(C4=CC=C(Cl)C=C4)N=3)C=C2)=O)C1
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| InChi Key |
LTOAWFRZXVPHAJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H19ClN4O4/c25-18-7-3-15(4-8-18)22-27-24(33-28-22)16-5-9-19(10-6-16)26-23(31)17-12-21(30)29(13-17)14-20-2-1-11-32-20/h1-11,17H,12-14H2,(H,26,31)
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| Chemical Name |
N-[4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]phenyl]-1-(furan-2-ylmethyl)-5-oxopyrrolidine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~270.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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