Synonym
PQ-912; PQ 912; PQ912; varoglutamstat
IUPAC/Chemical Name
(S)-1-(3H-Benzimidazol-5-yl)-5-(4-propoxyphenyl)imidazolidin-2-one
InChi Key
XHIKZWOEFZENIX-GOSISDBHSA-N
InChi Code
InChI=1S/C19H20N4O2/c1-2-9-25-15-6-3-13(4-7-15)18-11-20-19(24)23(18)14-5-8-16-17(10-14)22-12-21-16/h3-8,10,12,18H,2,9,11H2,1H3,(H,20,24)(H,21,22)/t18-/m1/s1
SMILES Code
O=C1NC[C@H](C2=CC=C(OCCC)C=C2)N1C3=CC=C4C(NC=N4)=C3
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
336.40
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: Scheltens P, Hallikainen M, Grimmer T, Duning T, Gouw AA, Teunissen CE, Wink AM, Maruff P, Harrison J, van Baal CM, Bruins S, Lues I, Prins ND. Safety, tolerability and efficacy of the glutaminyl cyclase inhibitor PQ912 in Alzheimer's disease: results of a randomized, double-blind, placebo-controlled phase 2a study. Alzheimers Res Ther. 2018 Oct 12;10(1):107. doi: 10.1186/s13195-018-0431-6. PubMed PMID: 30309389; PubMed Central PMCID: PMC6182869.
2: Pozzi C, Di Pisa F, Benvenuti M, Mangani S. The structure of the human glutaminyl cyclase-SEN177 complex indicates routes for developing new potent inhibitors as possible agents for the treatment of neurological disorders. J Biol Inorg Chem. 2018 Dec;23(8):1219-1226. doi: 10.1007/s00775-018-1605-1. Epub 2018 Aug 21. PubMed PMID: 30132075.
3: Hoffmann T, Meyer A, Heiser U, Kurat S, Böhme L, Kleinschmidt M, Bühring KU, Hutter-Paier B, Farcher M, Demuth HU, Lues I, Schilling S. Glutaminyl Cyclase Inhibitor PQ912 Improves Cognition in Mouse Models of Alzheimer's Disease-Studies on Relation to Effective Target Occupancy. J Pharmacol Exp Ther. 2017 Jul;362(1):119-130. doi: 10.1124/jpet.117.240614. Epub 2017 Apr 26. PubMed PMID: 28446518.
4: Lues I, Weber F, Meyer A, Bühring U, Hoffmann T, Kühn-Wache K, Manhart S, Heiser U, Pokorny R, Chiesa J, Glund K. A phase 1 study to evaluate the safety and pharmacokinetics of PQ912, a glutaminyl cyclase inhibitor, in healthy subjects. Alzheimers Dement (N Y). 2015 Oct 3;1(3):182-195. doi: 10.1016/j.trci.2015.08.002. eCollection 2015 Nov. PubMed PMID: 29854937; PubMed Central PMCID: PMC5975062.
