NF157

NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 μM, 170 μM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 μM), P2Y2 (Ki=28.9 μM), respectively[1]. NF157, significantly reduces expression of metalloproteinase (MMP) -3, MMP-13, can be used in the treatment of osteoarthritis (OA) [2].

Product Specifications

CAS Number

[104869-26-3]

UNSPSC

12352005

Target

P2Y Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/nf157.html

Purity

92.90

Solubility

H2O : 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1=CC(C(NC2=CC(C(NC3=CC=C(S(=O)(O[Na])=O)C4=CC(S(=O)(O[Na])=O)=CC(S(=O)(O[Na])=O)=C34)=O)=CC=C2F)=O)=CC=C1)NC5=CC(C(NC6=CC(C(NC7=CC=C(S(=O)(O[Na])=O)C8=CC(S(=O)(O[Na])=O)=CC(S(=O)(O[Na])=O)=C78)=O)=CC=C6F)=O)=CC=C5

Molecular Formula

C49H28F2N6Na6O23S6

Molecular Weight

1437.10

References & Citations

[1]Ullmann H, et al. Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. J Med Chem. 2005 Nov 3;48 (22) :7040-8.|[2]Wang D, et al. Inhibition of P2Y11R ameliorated TNF-α-induced degradation of extracellular matrix in human chondrocytic SW1353 cells. Am J Transl Res. 2019 Apr 15;11 (4) :2108-2116.