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RXFP1-Agonist-8
AOB4072
CAS No: 1482500-76-4
Chemical Name: 2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide; ML290; RXFP1-Agonist-8
915 Items
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| Quantity | mg | Unit Price ($/mg or $/Unit) | Final Price |
|---|---|---|---|
| 1 | 5 | $14.45 | Total: $72.25 |
| 1 | 10 | $12.24 | Total: $122.40 |
| 1 | 25 | $10.37 | Total: $259.25 |
| 1 | 50 | $8.84 | Total: $442.00 |
| 1 | 100 | $7.65 | Total: $765.00 |
Overview
The first potent and selective small-molecule agonist of human relaxin receptor 1 (RXFP1)
A cell-permeable 2-acetamido-N-phenylbenzamide that selectively activates human, but not mouse, LGR7/RXFP1-mediated cAMP induction (EC50 = 200 nM in THP1) via allosteric interaction with the ECL3 region without competing against ECL2-mediated relaxin binding or affecting AVPR1B- or LGR8/RXFP2-mediated cAMP induction. Although shown to be ~150-fold and 500-fold less potent than relaxin (RLX), respectively, in VEGF mRNA induction and cellular impedance assays, pharmacokinetic studies reveal superior in vivo stability to RLX and in vivo bioavailability in mice via oral (Cmax/Tmax = 604 nM/plasma/1 h and 1026 ng/g heart/1.5 h; 30 mg/kg) or intraperitoneal (Cmax/Tmax = 9.29 µM/plasma/1 h and 28.6 µmol/kg heart/1 h; 30 mg/kg) administration with good aqueous solubility (7 µM in PBS).
Reference:
1) Xiao, J., et al. 2013. Nat. Commun. 4, 1953.
Chemical Properties
| Molecular Formula | C24H21F3N2O5S |
| Molecular Weight | 506.49 |
| CAS Numbers | 1482500-76-4 |
| Solubility | DMSO |
| Stock Solution Guide | Aliquot and Freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| IUPAC/Chemical Name | 2-[[2-(1-methylethoxy)benzoyl]amino]-N-[3-[(trifluoromethyl)sulfonyl]phenyl]-benzamide |
| InChl Key | RSYHJSDOGMSLDH-UHFFFAOYSA-N |
| InChl Code | InChI=1S/C24H21F3N2O5S/c1-15(2)34-21-13-6-4-11-19(21)23(31)29-20-12-5-3-10-18(20)22(30)28-16-8-7-9-17(14-16)35(32,33)24(25,26)27/h3-15H,1-2H3,(H,28,30)(H,29,31) |
| SMILES Code | O=S(C1=CC=CC(NC(C2=CC=CC=C2NC(C3=C(OC(C)C)C=CC=C3)=O)=O)=C1)(C(F)(F)F)=O |
Storage and Handling
white powder at 4C for three years
Synonyms
ML290, ML-290, ML 290
References
1) Xiao, J., et al. Discovery, optimization, and biological activity of the first potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1). Probe Reports from the NIH Molecular Libraries Program (2012).
2) Diepenhorst, N.A.., et al. Investigation of interactions at the extracellular loops of the relaxin family peptide receptor 1 (RXFP1). J. Biol. Chem. 289(50), 34938-34952 (2014).
3) Huang, Z.,, et al. Activation of relaxin family receptor 1 from different mammalian species by relaxin peptide and small-molecule agonist ML290. Front. Endocrinol. (Lausanne) 6, 128 (2015).
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