A 412997 dihydrochloride |
Catalog No.GC14610 |
Selective D4 agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1347744-96-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
A 412997 dihydrochloride is a selective agonist of dopamine D4 receptor with Ki values of 7.9 and 12.1 nM for human and rat D4 receptors, respectively [1].
Dopamine D4 receptor is a G protein-coupled receptor and is activated by dopamine. It plays an important role in cognition, Parkinsons disease, addictive behaviors and so on.
A 412997 dihydrochloride is a selective dopamine D4 receptor agonist. In calcium flux functional assays, A-412997 activated the rat dopamine D4 receptor with EC50 value and intrinsic activity of 28.4 nM and 0.83, respectively [1].
In Spontaneous Hypertensive Rat pups (SHR pups), A 412997 significantly increased acquisition in the 5-trial repeated acquisition model. In the short-term social memory, A 412997 significantly shortened the second investigation time. In Wistar rats and Dawley rats, A 412997 (3 μM/kg, 10 μM/kg) increased locomotor activity [2]. In rats, A 412997 reduced non-rapid eye movement (NREM) sleep duration and increased waking duration. Also, A 412997 reduced rapid eye movement (REM) sleep duration and delayed the onset of REM sleep [3].
References:
[1]. Moreland RB, Patel M, Hsieh GC, et al. A-412997 is a selective dopamine D4 receptor agonist in rats. Pharmacol Biochem Behav, 2005, 82(1): 140-147.
[2]. Browman KE, Curzon P, Pan JB, et al. A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats. Pharmacol Biochem Behav, 2005, 82(1): 148-155.
[3]. Nakazawa S, Nakamichi K, Imai H, et al. Effect of dopamine D4 receptor agonists on sleep architecture in rats. Prog Neuropsychopharmacol Biol Psychiatry, 2015, 63: 6-13.
Cas No. | 1347744-96-0 | SDF | |
Chemical Name | (Z)-2-(4-(pyridin-2-yl)piperidin-1-yl)-N-(m-tolyl)acetimidic acid dihydrochloride | ||
Canonical SMILES | CC1=CC(/N=C(O)/CN2CCC(C3=CC=CC=N3)CC2)=CC=C1.Cl.Cl | ||
Formula | C19H23N3O.2HCl | M.Wt | 382.33 |
Solubility | <38.23mg/ml in Water; <19.12mg/ml in DMSO | Storage | Desiccate at RT |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6155 mL | 13.0777 mL | 26.1554 mL |
5 mM | 0.5231 mL | 2.6155 mL | 5.2311 mL |
10 mM | 0.2616 mL | 1.3078 mL | 2.6155 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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