Synonym
Way-120,491; Way120491; Way-120491; Way 120491; Celikalim
IUPAC/Chemical Name
2-(3-hydroxy-2,2-dimethyl-6-(trifluoromethoxy)chroman-4-yl)isoindolin-1-one
InChi Key
ZORATYFUTXFLJS-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H18F3NO4/c1-19(2)17(25)16(24-10-11-5-3-4-6-13(11)18(24)26)14-9-12(27-20(21,22)23)7-8-15(14)28-19/h3-9,16-17,25H,10H2,1-2H3
SMILES Code
O=C1N(C2C(O)C(C)(C)OC3=CC=C(OC(F)(F)F)C=C23)CC4=C1C=CC=C4
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, not in water
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
393.36
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: de Lorenzi FG. Celikalim (WAY-120491) increases K+ outward flux in dog and human airway smooth muscle. Pulm Pharmacol. 1994 Apr;7(2):129-35. PubMed PMID: 8081073.
2: Wojdan A, Freeden C, Woods M, Oshiro G, Spinelli W, Colatsky TJ, Sheldon JH, Norton NW, Warga D, Antane MM, Antane SA, Butera JA, Argentieri TM. Comparison of the potassium channel openers, WAY-133537, ZD6169, and celikalim on isolated bladder tissue and In vivo bladder instability in rat. J Pharmacol Exp Ther. 1999 Jun;289(3):1410-8. PubMed PMID: 10336534.
3: Furspan PB. WAY 120,491 activates ATP-sensitive potassium channels in rat tail artery. Eur J Pharmacol. 1992 Nov 17;223(2-3):201-3. PubMed PMID: 1478268.
4: Evans JM, Smith RJ, Stemp G. Separation of the enantiomers of some potassium channel activators using an alpha 1-acid glycoprotein column. J Chromatogr. 1992 Oct 9;623(1):163-7. PubMed PMID: 1452627.
5: Kitzen JM, McCallum JD, Harvey C, Morin ME, Oshiro GT, Colatsky TJ. Potassium channel activators cromakalim and celikalim (WAY-120,491) fail to decrease myocardial infarct size in the anesthetized canine. Pharmacology. 1992;45(2):71-82. PubMed PMID: 1523216.
6: Hohman TC, Cotter MA, Cameron NE. ATP-sensitive K(+) channel effects on nerve function, Na(+), K(+) ATPase, and glutathione in diabetic rats. Eur J Pharmacol. 2000 Jun 2;397(2-3):335-41. PubMed PMID: 10844132.
7: Patelunas-Hoffman DM, Carmint WJ, Colatsky TJ, Fenichel RL. Analysis of the potassium channel openers celikalim, pinacidil and cromakalim in platelet models of thrombosis. Thromb Res. 1994 Jun 1;74(5):441-52. PubMed PMID: 8085245.
8: Lodge NJ, Colatsky TJ, Cullinan CA, Follmer CH. Electromechanical effects of the putative potassium channel activator celikalim (WAY-120,491) on feline atrial and ventricular muscle. J Pharmacol Exp Ther. 1992 Jun;261(3):1153-9. PubMed PMID: 1602381.
9: Lodge NJ, Cohen RB, Havens CN, Colatsky TJ. The effects of the putative potassium channel activator WAY-120,491 on 86Rb efflux from the rabbit aorta. J Pharmacol Exp Ther. 1991 Feb;256(2):639-44. PubMed PMID: 1899702.
