Synonym
I-191; I191; I 191; MDK-2258; MDK 2258; MDK2258;
IUPAC/Chemical Name
4-(8-(tert-Butyl)-6-(4-fluorophenyl)imidazo[1,2-b]pyridazine-2-carbonyl)-3,3-dimethylpiperazin-2-one
InChi Key
DTASTQAQBOZSRR-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H26FN5O2/c1-22(2,3)16-12-17(14-6-8-15(24)9-7-14)27-29-13-18(26-19(16)29)20(30)28-11-10-25-21(31)23(28,4)5/h6-9,12-13H,10-11H2,1-5H3,(H,25,31)
SMILES Code
O=C1NCCN(C(C2=CN3N=C(C4=CC=C(F)C=C4)C=C(C(C)(C)C)C3=N2)=O)C1(C)C
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
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
423.49
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: Jiang Y, Yau MK, Lim J, Wu KC, Xu W, Suen JY, Fairlie DP. A Potent Antagonist
of Protease-Activated Receptor 2 That Inhibits Multiple Signaling Functions in
Human Cancer Cells. J Pharmacol Exp Ther. 2018 Feb;364(2):246-257. doi:
10.1124/jpet.117.245027. Epub 2017 Dec 20. PMID: 29263243.
2: Mogren S, Berlin F, Ramu S, Sverrild A, Porsbjerg C, Uller L, Andersson CK.
Mast cell tryptase enhances wound healing by promoting migration in human
bronchial epithelial cells. Cell Adh Migr. 2021 Dec;15(1):202-214. doi:
10.1080/19336918.2021.1950594. PMID: 34308764; PMCID: PMC8312598.
3: Jiang Y, Lim J, Wu KC, Xu W, Suen JY, Fairlie DP. PAR2 induces ovarian cancer
cell motility by merging three signalling pathways to transactivate EGFR. Br J
Pharmacol. 2021 Feb;178(4):913-932. doi: 10.1111/bph.15332. Epub 2020 Dec 30.
PMID: 33226635.
4: Nishimoto R, Kodama C, Yamashita H, Hattori F. Human Induced Pluripotent Stem
Cell-Derived Keratinocyte-Like Cells for Research on Protease-Activated Receptor
2 in Nonhistaminergic Cascades of Atopic Dermatitis . J Pharmacol Exp Ther. 2023
Feb;384(2):248-253. doi: 10.1124/jpet.122.001412. Epub 2022 Nov 9. PMID:
36351795.
5: Iyer A, Humphries TLR, Owens EP, Zhao KN, Masci PP, Johnson DW, Nikolic-
Paterson D, Gobe GC, Fairlie DP, Vesey DA. PAR2 Activation on Human Kidney
Tubular Epithelial Cells Induces Tissue Factor Synthesis, That Enhances Blood
Clotting. Front Physiol. 2021 Mar 10;12:615428. doi: 10.3389/fphys.2021.615428.
PMID: 33776786; PMCID: PMC7987918.
6: Humphries TLR, Shen K, Iyer A, Johnson DW, Gobe GC, Nikolic-Paterson D,
Fairlie DP, Vesey DA. PAR2-Induced Tissue Factor Synthesis by Primary Cultures
of Human Kidney Tubular Epithelial Cells Is Modified by Glucose Availability.
Int J Mol Sci. 2021 Jul 14;22(14):7532. doi: 10.3390/ijms22147532. PMID:
34299151; PMCID: PMC8304776.
