ML 221

Apelin receptor (APJ) antagonist CAS# 877636-42-5

ML 221

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ML 221

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Chemical Properties of ML 221

Cas No. 877636-42-5 SDF Download SDF
PubChem ID 7217941 Appearance Powder
Formula C17H11N3O6S M.Wt 385.35
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 31 mg/mL (80.45 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name [4-oxo-6-(pyrimidin-2-ylsulfanylmethyl)pyran-3-yl] 4-nitrobenzoate
SMILES C1=CN=C(N=C1)SCC2=CC(=O)C(=CO2)OC(=O)C3=CC=C(C=C3)[N+](=O)[O-]
Standard InChIKey UASIRTUMPRQVFY-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H11N3O6S/c21-14-8-13(10-27-17-18-6-1-7-19-17)25-9-15(14)26-16(22)11-2-4-12(5-3-11)20(23)24/h1-9H,10H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ML 221

DescriptionApelin receptor (APJ) antagonist (IC50 values are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively). Displays >37-fold selectivity over the closely related angiotensin II type 1 (AT1) receptor. Exhibits no toxicity towards human hepatocytes at concentrations >50 μM.

ML 221 Dilution Calculator

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ML 221 Molarity Calculator

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Preparing Stock Solutions of ML 221

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.595 mL 12.9752 mL 25.9504 mL 51.9009 mL 64.8761 mL
5 mM 0.519 mL 2.595 mL 5.1901 mL 10.3802 mL 12.9752 mL
10 mM 0.2595 mL 1.2975 mL 2.595 mL 5.1901 mL 6.4876 mL
50 mM 0.0519 mL 0.2595 mL 0.519 mL 1.038 mL 1.2975 mL
100 mM 0.026 mL 0.1298 mL 0.2595 mL 0.519 mL 0.6488 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on ML 221

Resveratrol attenuates ICAM-1 expression and monocyte adhesiveness to TNF-alpha-treated endothelial cells: evidence for an anti-inflammatory cascade mediated by the miR-221/222/AMPK/p38/NF-kappaB pathway.[Pubmed:28338009]

Sci Rep. 2017 Mar 24;7:44689.

Resveratrol, an edible polyphenolic phytoalexin, improves endothelial dysfunction and attenuates inflammation. However, the mechanisms have not been thoroughly elucidated. Therefore, we investigated the molecular basis of the effects of resveratrol on TNF-alpha-induced ICAM-1 expression in HUVECs. The resveratrol treatment significantly attenuated the TNF-alpha-induced ICAM-1 expression. The inhibition of p38 phosphorylation mediated the reduction in ICAM-1 expression caused by resveratrol. Resveratrol also decreased TNF-alpha-induced IkappaB phosphorylation and the phosphorylation, acetylation, and translocation of NF-kappaB p65. Moreover, resveratrol induced the AMPK phosphorylation and the SIRT1 expression in TNF-alpha-treated HUVECs. Furthermore, TNF-alpha significantly suppressed miR-221/-222 expression, which was reversed by resveratrol. miR-221/-222 overexpression decreased p38/NF-kappaB and ICAM-1 expression, which resulted in reduced monocyte adhesion to TNF-alpha-treated ECs. In a mouse model of acute TNF-alpha-induced inflammation, resveratrol effectively attenuated ICAM-1 expression in the aortic ECs of TNF-alpha-treated wild-type mice. These beneficial effects of resveratrol were lost in miR-221/222 knockout mice. Our data showed that resveratrol counteracted the TNF-alpha-mediated reduction in miR-221/222 expression and decreased the TNF-alpha-induced activation of p38 MAPK and NF-kappaB, thereby suppressing ICAM-1 expression and monocyte adhesion. Collectively, our results show that resveratrol attenuates endothelial inflammation by reducing ICAM-1 expression and that the protective effect was mediated partly through the miR-221/222/AMPK/p38/NF-kappaB pathway.

Overexpression of miRNA-221 promotes cell proliferation by targeting the apoptotic protease activating factor-1 and indicates a poor prognosis in ovarian cancer.[Pubmed:28350128]

Int J Oncol. 2017 Mar 7.

MicroRNAs are a class of small non-coding, endogenous RNAs involved in cancer development and progression. MicroRNA-221 (mir-221) has been reported to have both an oncogenic and tumor-suppressive role in human tumors, but the role of miR-221 in ovarian cancer is poorly understood. In the present study, the expression levels of miR-221 and the apoptosis protease activating factor 1 (APAF1) protein in 63 samples of ovarian cancer tissues and the cell lines, IOSE25, A2780, OVCAR3, SKOV3 and 3AO were detected by quantitative reverse-transcription polymerase chain reaction (qRT-PCR) and western blot analysis, respectively. Cell proliferation was measured using cell counting kit-8 (CCK-8); cell migration and invasion were detected using a transwell assay; cell apoptosis was evaluated by flow cytometry and hoechst staining, and a luciferase assay was performed to verify a putative target site of miR-221 in the 3'-UTR of APAF1 mRNA. Expression of miR-221 was upregulated in ovarian cancer tissues. Patients with increased miR-221 expression levels had a reduced disease-free survival (P=0.0014) and overall survival (P=0.0058) compared with those with low miR-221 expression. Transfection of SKOV3 and A2780 cell lines with miR-221 inhibitor induced APAF1 protein expression, suppressed cell proliferation and migration and promoted tumor cell apoptosis. In conclusion, the APAF1 gene was confirmed as a direct target of miR-221 and overexpression of APAF1 suppressed ovarian cancer cell proliferation and induced cell apoptosis in vitro. These findings indicate that miR-221-APAF1 should be studied further as a potential new diagnostic or prognostic biomarker for ovarian cancer.

miRNA-101-1 and miRNA-221 expressions and their polymorphisms as biomarkers for early diagnosis of hepatocellular carcinoma.[Pubmed:28366737]

Infect Genet Evol. 2017 Jul;51:173-181.

BACKGROUND: Hepatocellular carcinoma (HCC) is the fifth most common malignant tumor with an increasing incidence. Hepatitis C virus (HCV) is one of the major risk factors that lead to HCC development. MicroRNAs are conserved non-coding RNAs which regulate gene expression at the posttranscriptional level. They have been recently identified as important regulators that affect carcinogenesis. Of these miRNAs, are miR-221 and miR-101-1, which their aberrant expressions have been reported to play an important role in HCC. PATIENTS AND METHODS: In this study, we investigated the association between miR-221 and miR-101-1 polymorphisms and their expressions and the early prediction of HCC in HCV infected patients. Quantitative real-time PCR (qPCR) was done to estimate the expression levels of miRNA-221 and miRNA-101-1 in serum. To detect the genotyping of miR-221 and miR-101-1 related SNPs, DNA was extracted. Then, genotyping was performed using real-time PCR. RESULTS: We found that rs7536540 polymorphism in miR-101-1 is significantly associated with development of HCC. In addition, our results showed no significant association between rs17084733 polymorphism in miR-221 and HCC occurrence. We confirmed the upregulation of miR-221 and the downregulation of miR-101-1 in HCC. As regards HCV patients, miR-221and miR-101-1 were found to be upregulated. CONCLUSION: Both miR-221 and miR-101-1 expression levels may be useful as noninvasive diagnostic biomarkers for early prediction of HCC among HCV patients.

Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.[Pubmed:23010269]

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60.

The recently discovered apelin/APJ system has emerged as a critical mediator of cardiovascular homeostasis and is associated with the pathogenesis of cardiovascular disease. A role for apelin/APJ in energy metabolism and gastrointestinal function has also recently emerged. We disclose the discovery and characterization of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221), a potent APJ functional antagonist in cell-based assays that is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor. ML221 was derived from an HTS of the ~330,600 compound MLSMR collection. This antagonist showed no significant binding activity against 29 other GPCRs, except to the kappa-opioid and benzodiazepinone receptors (<50/<70%I at 10 muM). The synthetic methodology, development of structure-activity relationship (SAR), and initial in vitro pharmacologic characterization are also presented.

Description

ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.

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