Synonym
DQP-1105; DQP 1105; DQP1105
IUPAC/Chemical Name
4-[3-(4-bromophenyl)-5-(6-methyl-2-oxo-4-phenyl-3H-quinolin-3-yl)-3,4-dihydropyrazol-2-yl]-4-oxobutanoic acid
InChi Key
ACUGSRUCGXYFTL-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H24BrN3O4/c1-17-7-12-22-21(15-17)27(19-5-3-2-4-6-19)28(29(37)31-22)23-16-24(18-8-10-20(30)11-9-18)33(32-23)25(34)13-14-26(35)36/h2-12,15,24,28H,13-14,16H2,1H3,(H,35,36)
SMILES Code
O=C(O)CCC(N1N=C(C2C(N=C3C=CC(C)=CC3=C2C4=CC=CC=C4)=O)CC1C5=CC=C(Br)C=C5)=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
Biological target:
DQP-1105 is a potent noncompetitive NMDA receptor antagonist.
In vitro activity:
DQP-1105 inhibited GluN2C- and GluN2D-containing receptors with IC(50) values that were at least 50-fold lower than those for recombinant GluN2A-, GluN2B-, GluA1-, or GluK2-containing receptors. DQP-1105 inhibited single-channel currents in excised outside-out patches without significantly changing mean open time or single-channel conductance, suggesting that DQP inhibits a pregating step without changing the stability of the open pore conformation and thus channel closing rate.
Reference: Mol Pharmacol. 2011 Nov;80(5):782-95. https://pubmed.ncbi.nlm.nih.gov/21807990/
In vivo activity:
In vivo recordings from the STN of anesthetized adult rats demonstrated that the spike firing rate was increased by the GluN2C/D potentiator CIQ and decreased by the GluN2C/D antagonist DQP-1105, suggesting that NMDA receptor activity can influence STN output.
Reference: J Neurosci. 2015 Dec 2;35(48):15971-83. https://pubmed.ncbi.nlm.nih.gov/26631477/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
33.4 |
59.85 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
558.43
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 |
Formulation protocol:
1. Wu YN, Johnson SW. Memantine selectively blocks extrasynaptic NMDA receptors in rat substantia nigra dopamine neurons. Brain Res. 2015 Apr 7;1603:1-7. doi: 10.1016/j.brainres.2015.01.041. Epub 2015 Feb 2. PMID: 25656790.
2. Acker TM, Yuan H, Hansen KB, Vance KM, Ogden KK, Jensen HS, Burger PB, Mullasseril P, Snyder JP, Liotta DC, Traynelis SF. Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators. Mol Pharmacol. 2011 Nov;80(5):782-95. doi: 10.1124/mol.111.073239. Epub 2011 Aug 1. PMID: 21807990; PMCID: PMC3198917.
3. Swanger SA, Vance KM, Pare JF, Sotty F, Fog K, Smith Y, Traynelis SF. NMDA Receptors Containing the GluN2D Subunit Control Neuronal Function in the Subthalamic Nucleus. J Neurosci. 2015 Dec 2;35(48):15971-83. doi: 10.1523/JNEUROSCI.1702-15.2015. PMID: 26631477; PMCID: PMC4666920.
In vitro protocol:
1. Wu YN, Johnson SW. Memantine selectively blocks extrasynaptic NMDA receptors in rat substantia nigra dopamine neurons. Brain Res. 2015 Apr 7;1603:1-7. doi: 10.1016/j.brainres.2015.01.041. Epub 2015 Feb 2. PMID: 25656790.
2. Acker TM, Yuan H, Hansen KB, Vance KM, Ogden KK, Jensen HS, Burger PB, Mullasseril P, Snyder JP, Liotta DC, Traynelis SF. Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators. Mol Pharmacol. 2011 Nov;80(5):782-95. doi: 10.1124/mol.111.073239. Epub 2011 Aug 1. PMID: 21807990; PMCID: PMC3198917.
In vivo protocol:
1. Swanger SA, Vance KM, Pare JF, Sotty F, Fog K, Smith Y, Traynelis SF. NMDA Receptors Containing the GluN2D Subunit Control Neuronal Function in the Subthalamic Nucleus. J Neurosci. 2015 Dec 2;35(48):15971-83. doi: 10.1523/JNEUROSCI.1702-15.2015. PMID: 26631477; PMCID: PMC4666920.
1: Wu YN, Johnson SW. Memantine selectively blocks extrasynaptic NMDA receptors in rat substantia nigra dopamine neurons. Brain Res. 2015 Apr 7;1603:1-7. doi: 10.1016/j.brainres.2015.01.041. PubMed PMID: 25656790.
2: Lozovaya N, Gataullina S, Tsintsadze T, Tsintsadze V, Pallesi-Pocachard E, Minlebaev M, Goriounova NA, Buhler E, Watrin F, Shityakov S, Becker AJ, Bordey A, Milh M, Scavarda D, Bulteau C, Dorfmuller G, Delalande O, Represa A, Cardoso C, Dulac O, Ben-Ari Y, Burnashev N. Selective suppression of excessive GluN2C expression rescues early epilepsy in a tuberous sclerosis murine model. Nat Commun. 2014 Aug 1;5:4563. doi: 10.1038/ncomms5563. PubMed PMID: 25081057; PubMed Central PMCID: PMC4143949.
