Emapticap pegol 是促炎趋化因子 C-C 基序配体 2 (CCL2) 的抑制剂。Emapticap pegol 是一种 40 个核苷酸的寡核苷酸适体，在人 (NOX-E36) 和小鼠 (mNOX-E36) 中具有不同的 Spiegelmers (L-RNA 适配子) 形式。
| 生物活性 | Emapticap pegol is a inhibitor of pro-inflammatorychemokine 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] |
体外研究
(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; andmNOX-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].
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体内研究
(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: | 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. |
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| Clinical Trial | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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