DQP-1105 | CAS#380560-89-4

DQP-1105
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531764

CAS#: 380560-89-4

Description: DQP-1105 is a negative allosteric modulator of the GluN2C/D NMDA receptor inhibiting receptor function more potently when glutamate is present .

Chemical Structure

DQP-1105

CAS# 380560-89-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531764
Name: DQP-1105
CAS#: 380560-89-4
Chemical Formula: C29H24BrN3O4
Exact Mass: 557.10
Molecular Weight: 558.432
Elemental Analysis: C, 62.37; H, 4.33; Br, 14.31; N, 7.52; O, 11.46

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 355	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Appearance: Solid powder

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

More Info:

Product Data:

Product Data

Instruction:

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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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	33.4	59.85

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.

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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.

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