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Emapticap pegol (Synonyms: NOX-E36)

Cat. No.: HY-148100
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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).

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Emapticap pegol Chemical Structure

Emapticap pegol Chemical Structure

CAS No. : 1390630-22-4

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Description

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].

IC50 & Target

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

In Vitro

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].

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

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].

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

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: Male Apoe KO 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.
CAS No.
SMILES

[Emapticap pegol]

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Emapticap pegol
Cat. No.:
HY-148100
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