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Emapticap pegol

Product NameEmapticap pegol
CAS1390630-22-4
MF
MW0
EINECS
MOL FileMol File

Chemical Properties

Sequence

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)

Usage And Synthesis

Uses

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].

in vivo

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].

Animal Model:	Non-irradiated immunocompetent C57BL/6 mice injected with syngeneic AML1/ETO9a-expressing primary murine leukemia cells^[2]
Dosage:	14.4 mg/kg (mNOX-E36, Emapticap pegol of the mouse-specific CCL2 Spiegelmer)
Administration:	Subcutaneous injection; three times per week for 3 weeks
Result:	Abrogated this macrophage infiltration within the leukemia microenvironment.

Animal Model:	MaleApoeKO C57BL/6J mice rendered diabetic (6-week-old)^[3]
Dosage:	20 mg/kg (mNOX-E36, Emapticap pegol of the mouse-specific CCL2 Spiegelmer)
Administration:	Subcutaneous injection; three times per week for 4 weeks
Result:	Reduced albumin/creatinine ratio without affecting blood glucose level and weight of mice. Reduced heparanase and cathepsin L expression.

References

[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. DOI:10.1093/ndt/gfv459
[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. DOI:10.1016/j.ajpath.2017.07.020

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