Synonym
ZK-187638; ZK 187638; ZK187638
IUPAC/Chemical Name
2,3-Dimethyl-6-phenyl-12H-[1,3]dioxolo[4,5-h]imidazo[1,2-c][2,3]benzodiazepine
InChi Key
ZFQASTCWCGRURV-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H17N3O2/c1-12-13(2)23-19(21-12)9-15-8-17-18(25-11-24-17)10-16(15)20(22-23)14-6-4-3-5-7-14/h3-8,10H,9,11H2,1-2H3
SMILES Code
CC1=C(C)N=C2N1N=C(C3=CC=CC=C3)C4=CC(OCO5)=C5C=C4C2
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
331.38
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: Elger B, Gieseler M, Schmuecker O, Schumann I, Seltz A, Huth A. Extended therapeutic time window after focal cerebral ischemia by non-competitive inhibition of AMPA receptors. Brain Res. 2006 Apr 26;1085(1):189-94. Epub 2006 Apr 3. PubMed PMID: 16580649.
2: Elger B, Huth A, Neuhaus R, Ottow E, Schneider H, Seilheimer B, Turski L. Novel alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration. J Med Chem. 2005 Jul 14;48(14):4618-27. PubMed PMID: 15999999.
3: Tortarolo M, Grignaschi G, Calvaresi N, Zennaro E, Spaltro G, Colovic M, Fracasso C, Guiso G, Elger B, Schneider H, Seilheimer B, Caccia S, Bendotti C. Glutamate AMPA receptors change in motor neurons of SOD1G93A transgenic mice and their inhibition by a noncompetitive antagonist ameliorates the progression of amytrophic lateral sclerosis-like disease. J Neurosci Res. 2006 Jan;83(1):134-46. PubMed PMID: 16323214.
4: Elger B, Schneider M, Winter E, Carvelli L, Bonomi M, Fracasso C, Guiso G, Colovic M, Caccia S, Mennini T. Optimized synthesis of AMPA receptor antagonist ZK 187638 and neurobehavioral activity in a mouse model of neuronal ceroid lipofuscinosis. ChemMedChem. 2006 Oct;1(10):1142-8. PubMed PMID: 16972289.
