Synonym
Lexaptepid pegol;
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
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
Biological target:
Lexaptepid pegol is a structured mirror-image L-oligoribonucleotide known as a Spiegelmer.
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: Boyce M, Warrington S, Cortezi B, Zöllner S, Vauléon S, Swinkels DW, Summo L, Schwoebel F, Riecke K. Safety, pharmacokinetics and pharmacodynamics of the anti-hepcidin Spiegelmer lexaptepid pegol in healthy subjects. Br J Pharmacol. 2016 May;173(10):1580-8. doi: 10.1111/bph.13433. Epub 2016 Apr 8. PubMed PMID: 26773325; PubMed Central PMCID: PMC4842915.
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. Review. PubMed PMID: 25236655.
3: van Eijk LT, John AS, Schwoebel F, Summo L, Vauléon S, Zöllner S, Laarakkers CM, Kox M, van der Hoeven JG, Swinkels DW, Riecke K, Pickkers P. Effect of the antihepcidin Spiegelmer lexaptepid on inflammation-induced decrease in serum iron in humans. Blood. 2014 Oct 23;124(17):2643-6. doi: 10.1182/blood-2014-03-559484. Epub 2014 Aug 27. PubMed PMID: 25163699; PubMed Central PMCID: PMC4208279.
4: Steinbicker AU. A novel treatment of anemia of inflammation. Blood. 2014 Oct 23;124(17):2618-9. doi: 10.1182/blood-2014-09-599282. PubMed PMID: 25342662.
5: Testa U, Castelli G, Elvira P. Experimental and investigational therapies for chemotherapy-induced anemia. Expert Opin Investig Drugs. 2015;24(11):1433-45. doi: 10.1517/13543784.2015.1085505. Epub 2015 Sep 10. Review. PubMed PMID: 26359222.
6: Schwoebel F, van Eijk LT, Zboralski D, Sell S, Buchner K, Maasch C, Purschke WG, Humphrey M, Zöllner S, Eulberg D, Morich F, Pickkers P, Klussmann S. The effects of the anti-hepcidin Spiegelmer NOX-H94 on inflammation-induced anemia in cynomolgus monkeys. Blood. 2013 Mar 21;121(12):2311-5. doi: 10.1182/blood-2012-09-456756. Epub 2013 Jan 24. PubMed PMID: 23349391; PubMed Central PMCID: PMC3606066.
