MRS1754

MRS1754 is an adenosine A_2B receptor antagonist (K_i = 1.97 nM).¹ It is selective for adenosine A_2B receptors over adenosine A₁, A_2A, and A₃ receptors (K_is = 403, 503, and 570 nM, respectively). In vivo, MRS1754 (0.5-10 mg/kg) increases 28-day survival, as well as decreases peritoneal bacterial growth and plasma levels of IL-6, TNF-α, and MIP-2, in a mouse model of sepsis induced by cecal ligation and puncture (CLP).² MRS1754 (1 mg/kg) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).³

WARNING This product is not for human or veterinary use.

1. Kim, Y.-C., Ji, X.-d., Melman, N., et al. Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A2B adenosine receptors. J. Med. Chem. 43(6), 1165-1172 (2000).

2. Belikoff, B.G., Hatfield, S., Georgiev, P., et al. A2B adenosine receptor blockade enhances macrophage-mediated bacterial phagocytosis and improves polymicrobial sepsis survival in mice. J. Immunol. 186(4), 2444-2453 (2011).

3. Wei, W., Du, C., Lv, J., et al. Blocking A2B adenosine receptor alleviates pathogenesis of experimental autoimmune encephalomyelitis via inhibition of IL-6 production and Th17 differentiation. J. Immunol. 190(1), 138-146 (2013).