Emapticap pegol  (Synonyms: NOX-E36)

Emapticap pegol is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36)^[1][2][3].

chemokine C-C motif-ligand 2 (CCL2)^[1]; MCP-1^[3]

Spiegelmers are RNA-like molecules built from L-ribose units that are able to bind molecules such as peptides and proteins. NOX-E36, is human-specific CCL2 Spiegelmer; and mNOX-E36, is the mouse-specific CCL2 Spiegelmer^[2].
NOX-E36 (1 nM) significantly inhibits CCL2-mediated migration in human monocytic leukemia cell line THP-1^[2].
NOX-E36 inhibits monocyte chemotactic protein-1 (MCP-1), and blocks the inflammatory cell recruitment and differentiation of macrophages mediated by MCP-1^[3].
mNOX-E36 inhibits the migration and signaling pathway activation in murine hematopoietic cells, and blocks CCL2 receptor expressing Ba/F3 cells (Ba/F3-CCR2) migration (~2000 fold than normal migration) in a dose-dependent manner^[2].
mNOX-E36 abrogates the phosphorylation induced by CCL2 of AKT, ERK, p35-MAPK, respectively in mCCL2-stimulated cells (30 min)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Emapticap pegol (14.4 mg/kg, mNOX-E36; s.c.; three times per week, for 3 weeks) interferes the infiltration of M2-like macrophages into spleens of leukemia-bearing mice^[2].
Emapticap pegol (20 mg/kg, mNOX-E36; s.c.; three times per week, for 4 weeks) reduces albuminuria and restores the glomerular endothelial glycocalyx in diabetic mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1390630-22-4

Poly(oxy-1,2-ethanediyl), α-hydro-ω-methoxy-, 5′-ether with RNA β-L-(G-C-A-C-G-U-C-C-C-U-C-A-C-C-G-G-U-G-C-A-A-G-U-G-A-A-G-C-C-G-U-G-G-C-U-C-U-G-C-G) 5′-[6-[[2-[(2-hydroxyacetyl)(2-hydroxyethyl)amino]acetyl]amino]hexyl hydrogen phosphate] (2:1)

[Emapticap pegol]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Menne J, et al. C-C motif-ligand 2 inhibition with emapticap pegol (NOX-E36) in type 2 diabetic patients with albuminuria. Nephrol Dial Transplant. 2017 Feb 1;32(2):307-315.   [Content Brief]

  [2]. Rodrigo, et al. Effects of CCL2/CCR2 Blockade in Acute Myeloid Leukemia. Blood.

  [3]. Boels MGS, et al. Systemic Monocyte Chemotactic Protein-1 Inhibition Modifies Renal Macrophages and Restores Glomerular Endothelial Glycocalyx and Barrier Function in Diabetic Nephropathy. Am J Pathol. 2017 Nov;187(11):2430-2440.   [Content Brief]