| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Pro-inflammatory chemokine C-C motif-ligand 2 (CCL2/MCP-1); Spiegelmers are RNA-like molecules built from L-ribose units that bind target proteins with high affinity.
|
|---|---|
| ln Vitro |
NOX-E36 (1 nM) significantly inhibits CCL2-mediated migration in the human monocytic leukemia cell line THP-1. mNOX-E36 blocks CCL2 receptor-expressing Ba/F3 cell migration (~2000-fold reduction) and abrogates AKT, ERK, and p35-MAPK phosphorylation induced by CCL2.
|
| ln Vivo |
Emapticap pegol (mNOX-E36, 14.4 mg/kg, s.c., three times/week for 3 weeks) interferes with infiltration of M2-like macrophages into spleens of leukemia-bearing mice. At 20 mg/kg (s.c., three times/week for 4 weeks), it reduces albuminuria and restores the glomerular endothelial glycocalyx in diabetic mice.
|
| Enzyme Assay |
Not applicable; high-affinity binding is assessed via surface plasmon resonance (SPR) or competitive ELISA using immobilized CCL2 and the Spiegelmer; IC50 is determined by measuring inhibition of CCL2-mediated chemotaxis in transwell assays.
|
| Cell Assay |
THP-1 cells are placed in the upper chamber of a transwell plate; NOX-E36 (0.1-100 nM) and CCL2 are added; after 2-4 h, migrated cells in the lower chamber are counted; or Ba/F3-CCR2 cells are used in a similar chemotaxis assay.
|
| Animal Protocol |
Mouse model (C57BL/6 mice injected with AML1/ETO9a-expressing primary murine leukemia cells) or Apoe KO diabetic mice are used. Emapticap pegol (14.4 or 20 mg/kg) is administered subcutaneously three times per week; endpoints include macrophage infiltration (flow cytometry) and albumin/creatinine ratio (urine analysis).
|
| ADME/Pharmacokinetics |
PK properties of emapticap pegol have been evaluated in type 2 diabetic patients; as an oligonucleotide Spiegelmer, it is administered subcutaneously and exhibits a half-life suitable for three-times-weekly dosing.
|
| Toxicity/Toxicokinetics |
In a Phase 2 study in type 2 diabetic patients with albuminuria, emapticap pegol was generally safe and well tolerated. No serious toxicity concerns were reported; beneficial effects on albumin/creatinine ratio and HbA1c were observed.
|
| References | |
| Additional Infomation |
Emapticap pegol (NOX-E36) has completed Phase 2 clinical trials in type 2 diabetic patients with albuminuria (NCT01547897). It is not FDA/EMA approved. It is for research use only.
|
| Appearance |
Typically exists as solid at room temperature
|
|---|---|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
