TargetMol

ML221

Product Code:
 
TAR-T4390
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T4390-1mL1 mL * 10 mM (in DMSO)£111.00
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TAR-T4390-5mg5mg£111.00
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TAR-T4390-10mg10mg£133.00
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TAR-T4390-25mg25mg£206.00
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TAR-T4390-50mg50mg£277.00
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TAR-T4390-100mg100mg£446.00
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Further Information

Bioactivity:
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.
CAS:
877636-42-5
Formula:
C17H11N3O6S
Molecular Weight:
385.35
Pathway:
GPCR/G Protein
Purity:
0.9774
SMILES:
[O-][N+](=O)c1ccc(cc1)C(=O)Oc1coc(CSc2ncccn2)cc1=O
Target:
Apelin receptor

References

Maloney PR, etal. 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. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60. Ye L, Huang Y, Liu X, et al.Apelin/APJ system protects placental trophoblasts from hypoxia-induced oxidative stress through activating PI3K/Akt signaling pathway in preeclampsia.Free Radical Biology and Medicine.2023 Xiong M, Chen H, Fan Y, et al.Tubular Elabela-APJ axis attenuates ischemia-reperfusion induced acute kidney injury and the following AKI-CKD transition by protecting renal microcirculation.Theranostics.2023, 13(10): 3387.