WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H533244
CAS#: 1482500-76-4
Description: ML290 is a potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1).
Hodoodo Cat#: H533244
Name: ML290
CAS#: 1482500-76-4
Chemical Formula: C24H21F3N2O5S
Exact Mass: 506.11
Molecular Weight: 506.496
Elemental Analysis: C, 56.91; H, 4.18; F, 11.25; N, 5.53; O, 15.79; S, 6.33
Synonym: ML290; ML 290; ML-290.
IUPAC/Chemical Name: 2-[(2-propan-2-yloxybenzoyl)amino]-N-[3-(trifluoromethylsulfonyl)phenyl]benzamide
InChi Key: RSYHJSDOGMSLDH-UHFFFAOYSA-N
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)
SMILES Code: O=C(NC1=CC=CC(S(=O)(C(F)(F)F)=O)=C1)C2=CC=CC=C2NC(C3=CC=CC=C3OC(C)C)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 506.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Agoulnik AI, Agoulnik IU, Hu X, Marugan J. Synthetic non-peptide low molecular weight agonists of the relaxin receptor 1. Br J Pharmacol. 2016 Oct 23. doi: 10.1111/bph.13656. [Epub ahead of print] Review. PubMed PMID: 27771940.
2: Hu X, Myhr C, Huang Z, Xiao J, Barnaeva E, Ho BA, Agoulnik IU, Ferrer M, Marugan JJ, Southall N, Agoulnik AI. Structural Insights into the Activation of Human Relaxin Family Peptide Receptor 1 by Small-Molecule Agonists. Biochemistry. 2016 Mar 29;55(12):1772-83. doi: 10.1021/acs.biochem.5b01195. PubMed PMID: 26866459; PubMed Central PMCID: PMC5137375.
3: Huang Z, Myhr C, Bathgate RA, Ho BA, Bueno A, Hu X, Xiao J, Southall N, Barnaeva E, Agoulnik IU, Marugan JJ, Ferrer M, Agoulnik AI. Activation of Relaxin Family Receptor 1 from Different Mammalian Species by Relaxin Peptide and Small-Molecule Agonist ML290. Front Endocrinol (Lausanne). 2015 Aug 17;6:128. doi: 10.3389/fendo.2015.00128. PubMed PMID: 26347712; PubMed Central PMCID: PMC4538381.
4: Halls ML, Bathgate RA, Sutton SW, Dschietzig TB, Summers RJ. International Union of Basic and Clinical Pharmacology. XCV. Recent advances in the understanding of the pharmacology and biological roles of relaxin family peptide receptors 1-4, the receptors for relaxin family peptides. Pharmacol Rev. 2015;67(2):389-440. doi: 10.1124/pr.114.009472. Review. PubMed PMID: 25761609; PubMed Central PMCID: PMC4394689.
5: Diepenhorst NA, Petrie EJ, Chen CZ, Wang A, Hossain MA, Bathgate RA, Gooley PR. Investigation of interactions at the extracellular loops of the relaxin family peptide receptor 1 (RXFP1). J Biol Chem. 2014 Dec 12;289(50):34938-52. doi: 10.1074/jbc.M114.600882. PubMed PMID: 25352603; PubMed Central PMCID: PMC4263891.
6: Xiao J, Chen CZ, Huang Z, Agoulnik IU, Ferrer M, Southall N, Hu X, Zheng W, Agoulnik AI, Marugan JJ. Discovery, optimization, and biological activity of the first potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1). 2012 Mar 10 [updated 2013 May 8]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. Available from http://www.ncbi.nlm.nih.gov/books/NBK153218/ PubMed PMID: 23905199.