Synonym
Emapticap pegol; OXE36 free acid; OXE 36 free acid; OX-E36 free acid
IUPAC/Chemical Name
8-(2-(2-methoxyethoxy)ethyl)-7,10-dioxo-2,5-dioxa-8,11-diazaheptadecan-17-yl dihydrogen phosphate
InChi Key
QJAGBAPUFWBVSD-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H37N2O10P/c1-26-11-13-28-10-8-20(18(22)16-29-14-12-27-2)15-17(21)19-7-5-3-4-6-9-30-31(23,24)25/h3-16H2,1-2H3,(H,19,21)(H2,23,24,25)
SMILES Code
COCCOCCN(C(COCCOC)=O)CC(NCCCCCCOP(O)(O)=O)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
472.47
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Menne J, Eulberg D, Beyer D, Baumann M, Saudek F, Valkusz Z, Więcek A, Haller H; Emapticap Study Group. 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. PMID: 28186566; PMCID: PMC5410979.
2: Vater A, Klussmann S. Turning mirror-image oligonucleotides into drugs: the evolution of Spiegelmer(®) therapeutics. Drug Discov Today. 2015 Jan;20(1):147-55. doi: 10.1016/j.drudis.2014.09.004. Epub 2014 Sep 16. PMID: 25236655.
3: Perez-Gomez MV, Sanchez-Niño MD, Sanz AB, Zheng B, Martín-Cleary C, Ruiz- Ortega M, Ortiz A, Fernandez-Fernandez B. Targeting inflammation in diabetic kidney disease: early clinical trials. Expert Opin Investig Drugs. 2016 Sep;25(9):1045-58. doi: 10.1080/13543784.2016.1196184. Epub 2016 Jun 13. PMID: 27268955.
4: Oberthür D, Achenbach J, Gabdulkhakov A, Buchner K, Maasch C, Falke S, Rehders D, Klussmann S, Betzel C. Crystal structure of a mirror-image L-RNA aptamer (Spiegelmer) in complex with the natural L-protein target CCL2. Nat Commun. 2015 Apr 22;6:6923. doi: 10.1038/ncomms7923. PMID: 25901662; PMCID: PMC4423205.
5: Boels MGS, Koudijs A, Avramut MC, Sol WMPJ, Wang G, van Oeveren-Rietdijk AM, van Zonneveld AJ, de Boer HC, van der Vlag J, van Kooten C, Eulberg D, van den Berg BM, IJpelaar DHT, Rabelink TJ. 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. Epub 2017 Aug 22. PMID: 28837800.
