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G Protein-Coupled Receptor Ligands

ML290 View larger

RXFP1-Agonist-8

AOB4072

CAS No: 1482500-76-4

 

Chemical Name: 2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide; ML290; RXFP1-Agonist-8

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Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
1100 $7.65 Total: $765.00
150 $8.84 Total: $442.00
125 $10.37 Total: $259.25
110 $12.24 Total: $122.40
15 $14.45 Total: $72.25

Data sheet

Molecular FormulaC24H21F3N2O5S
Molecular Weight506.49
CAS Numbers1482500-76-4
Storage Conditionwhite powder at 4C for three years
SolubilityDMSO
Stock Solution GuideAliquot and Freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
SynonymML290, ML-290, ML 290
IUPAC/Chemical Name2-[[2-(1-methylethoxy)benzoyl]amino]-N-[3-[(trifluoromethyl)sulfonyl]phenyl]-benzamide
InChl KeyRSYHJSDOGMSLDH-UHFFFAOYSA-N
InChl CodeInChI=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 CodeO=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
References1) 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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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.

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