An RXFP1 agonist
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ML-290

Item No. 21134

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[2-(1-methylethoxy)benzoyl]amino]-N-[3-[(trifluoromethyl)sulfonyl]phenyl]-benzamide
CAS Number
1482500-76-4
Synonyms
  • RXFP1 Agonist 8​​
Molecular Formula
C24H21F3N2O5S
Formula Weight
506.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:2): 0.33 mg/mlDMSO: 25 mg/mlEthanol: 0.14 mg/ml
λmax
212, 263 nm
SMILES
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
InChi 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)
InChi Key
RSYHJSDOGMSLDH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    ML-290 is an allosteric agonist of relaxin family peptide receptor 1 (RXFP1; EC50 = 0.094 µM for the human receptor in a cAMP produciton assay).1 It is selective for RXFP1 over RXFP2 (EC50 = 1.5 µM). ML-90 (250 nM) induces expression of VEGF in THP-1 cells expressing human RXFP1. It stimulates cAMP release from HEK293 cells expressing the human, macaque, pig, or rabbit receptors, but not the guinea pig or mouse receptors.2 ML-290 (5 µM) increases the expression of MMP1 and PPARGC1A and decreases COL1A1 expression in primary human hepatic stellate cells.3 It reduces carbon tetrachloride-induced liver fibrosis in transgenic mice expressing human RXFP1 when administered at a dose of 37 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xiao, J., Chen, C.Z., Huang, Z., 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. Huang, Z., Myhr, C., Bathgate, R.A.D., 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).

    3. Kaftanovskaya, E.M., Ng, H.H., Soula, M., et al. Therapeutic effects of a small molecule agonist of the relaxin receptor ML290 in liver fibrosis. FASEB J. 33(11), 12435-12446 (2019).