Synonym
KRP-109; KRP 109; KRP109;
IUPAC/Chemical Name
2-[2-(3-Dimethylamino-pyrrolidin-1-yl)-pyridin-3-yl]-5-ethyl-7-methoxy-benzo[d][1,3]oxazin-4-one Maleate
InChi Key
YLFBWXUNSRKFNI-BTJKTKAUSA-N
InChi Code
InChI=1S/C22H26N4O3.C4H4O4/c1-5-14-11-16(28-4)12-18-19(14)22(27)29-21(24-18)17-7-6-9-23-20(17)26-10-8-15(13-26)25(2)3;5-3(6)1-2-4(7)8/h6-7,9,11-12,15H,5,8,10,13H2,1-4H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
SMILES Code
O=C1C2=C(CC)C=C(OC)C=C2N=C(C3=CC=CN=C3N4CC(N(C)C)CC4)O1.O=C(O)/C=C\C(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
>2 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
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
510.54
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: Chillappagari S, Müller C, Mahavadi P, Guenther A, Nährlich L, Rosenblum J, Rubin BK, Henke MO. A small molecule neutrophil elastase inhibitor, KRP-109, inhibits cystic fibrosis mucin degradation. J Cyst Fibros. 2016 May;15(3):325-31. doi: 10.1016/j.jcf.2015.10.008. Epub 2015 Oct 30. PubMed PMID: 26526358.
2: Yamada K, Yanagihara K, Araki N, Harada Y, Morinaga Y, Izumikawa K, Kakeya H, Yamamoto Y, Hasegawa H, Kohno S, Kamihira S. In vivo efficacy of KRP-109, a novel elastase inhibitor, in a murine model of severe pneumococcal pneumonia. Pulm Pharmacol Ther. 2011 Dec;24(6):660-5. doi: 10.1016/j.pupt.2011.08.001. Epub 2011 Aug 16. PubMed PMID: 21864700.
