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JP 1302 dihydrochloride

CAS# 1259314-65-2

JP 1302 dihydrochloride

Catalog No. BCC7449----Order now to get a substantial discount!

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JP 1302 dihydrochloride: 5mg $127 In Stock
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Chemical structure

JP 1302 dihydrochloride

3D structure

Chemical Properties of JP 1302 dihydrochloride

Cas No. 1259314-65-2 SDF Download SDF
PubChem ID 49855035 Appearance Powder
Formula C24H26Cl2N4 M.Wt 441.4
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 5 mM in DMSO
Chemical Name N-[4-(4-methylpiperazin-1-yl)phenyl]acridin-9-amine;dihydrochloride
SMILES CN1CCN(CC1)C2=CC=C(C=C2)NC3=C4C=CC=CC4=NC5=CC=CC=C53.Cl.Cl
Standard InChIKey VVZOADYFJAJZGL-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H24N4.2ClH/c1-27-14-16-28(17-15-27)19-12-10-18(11-13-19)25-24-20-6-2-4-8-22(20)26-23-9-5-3-7-21(23)24;;/h2-13H,14-17H2,1H3,(H,25,26);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of JP 1302 dihydrochloride

Descriptionα2C-adrenoceptor antagonist that displays ~ 50-fold selectivity over other α2-adrenoceptor subtypes (Ki values are 28, 1470, 1700 and 3150 nM for human α2C, α2B, α2D and α2A subtypes respectively). Potently antagonizes adrenalin-stimulated 35GTPγS binding in vitro (KB = 16 nM) and produces antidepressant and antipsychotic-like effects in vivo.

JP 1302 dihydrochloride Dilution Calculator

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JP 1302 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of JP 1302 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2655 mL 11.3276 mL 22.6552 mL 45.3104 mL 56.638 mL
5 mM 0.4531 mL 2.2655 mL 4.531 mL 9.0621 mL 11.3276 mL
10 mM 0.2266 mL 1.1328 mL 2.2655 mL 4.531 mL 5.6638 mL
50 mM 0.0453 mL 0.2266 mL 0.4531 mL 0.9062 mL 1.1328 mL
100 mM 0.0227 mL 0.1133 mL 0.2266 mL 0.4531 mL 0.5664 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on JP 1302 dihydrochloride

Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302.[Pubmed:17220913]

Br J Pharmacol. 2007 Feb;150(4):391-402.

BACKGROUND AND PURPOSE: Pharmacological validation of novel functions for the alpha2A-, alpha2B-, and alpha2C-adrenoceptor (AR) subtypes has been hampered by the limited specificity and subtype-selectivity of available ligands. The current study describes a novel highly selective alpha2C-adrenoceptor antagonist, JP-1302 (acridin-9-yl-[4-(4-methylpiperazin-1-yl)-phenyl]amine). EXPERIMENTAL APPROACH: Standard in vitro binding and antagonism assays were employed to demonstrate the alpha2C-AR specificity of JP-1302. In addition, JP-1302 was tested in the forced swimming test (FST) and the prepulse-inhibition of startle reflex (PPI) model because mice with genetically altered alpha2C-adrenoceptors have previously been shown to exhibit different reactivity in these tests when compared to wild-type controls. KEY RESULTS: JP-1302 displayed antagonism potencies (KB values) of 1,500, 2,200 and 16 nM at the human alpha2A-, alpha2B-, and alpha2C-adrenoceptor subtypes, respectively. JP-1302 produced antidepressant and antipsychotic-like effects, i.e. it effectively reduced immobility in the FST and reversed the phencyclidine-induced PPI deficit. Unlike the alpha2-subtype non-selective antagonist atipamezole, JP-1302 was not able to antagonize alpha2-agonist-induced sedation (measured as inhibition of spontaneous locomotor activity), hypothermia, alpha2-agonist-induced mydriasis or inhibition of vas deferens contractions, effects that have been generally attributed to the alpha2A-adrenoceptor subtype. In contrast to JP-1302, atipamezole did not antagonize the PCP-induced prepulse-inhibition deficit. CONCLUSIONS AND IMPLICATIONS: The results provide further support for the hypothesis that specific antagonism of the alpha2C-adrenoceptor may have therapeutic potential as a novel mechanism for the treatment of neuropsychiatric disorders.

JP-1302: a new tool to shed light on the roles of alpha2C-adrenoceptors in brain.[Pubmed:17220912]

Br J Pharmacol. 2007 Feb;150(4):381-2.

The discovery of JP-1302 as a selective, high affinity antagonist at the alpha2C-adrenoceptor will enable researchers to probe the functional role and address the therapeutic utility of this potentially highly important adrenoceptor subtype.

Description

JP1302 dihydrochloride is a selective, high affinity antagonist of the alpha2C-adrenoceptor (α2C-adrenoceptor), with a Kb value (antagonist activity) of 16 nM and a Ki (binding affinity) value of 28 nM.

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