RO5166017 |
Katalog-Nr.GC48912
One-Click Copy Product Info
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RO5166017 ist ein oral aktiver und artÜbergreifender TAAR1-Agonist mit Ki-Werten von 1,9 nM, 2,7 nM, 31 nM und 24 nM fÜr Maus, Ratte, Mensch bzw. Cynomolgus-Affe.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1048346-74-2
Sample solution is provided at 25 µL, 10mM.
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RO5166017 is an agonist of trace amine-associated receptor 1 (TAAR1).1 It binds to TAAR1 (Kis = 31, 24, 1.9, and 2.7 nM in HEK293 cells expressing the recombinant human, cynomolgus monkey, mouse, or rat receptor, respectively) and is greater than 15-fold selective for TAAR1 over a panel of 123 receptors, ion channels, and transporters at 10 µM. RO5166017 induces cAMP production in HEK293 cells expressing the recombinant human, cynomolgus monkey, mouse, or rat TAAR1 (EC50s = 55, 97, 3.3, and 14 nM, respectively). It reduces the frequency of neuronal firing in mouse ventral tegmental area (VTA) and dorsal raphe nucleus (DRN) slices (IC50s = 1.73 and 2.99 nM, respectively), which endogenously express high levels of dopaminergic and serotonergic neurons, respectively. RO5166017 (0.3 mg/kg) inhibits stress-induced hyperthermia, indicating anxiolytic-like activity, as well as reduces cocaine-induced hyperlocomotion, in mice. It also impairs expression, but not reconsolidation, of cocaine-induced place preference in rats.2
1.Revel, F.G., Moreau, J.-L., Gainetdinov, R.R., et al.TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activityProc. Natl. Acad. Sci. USA108(20)8485-8490(2011) 2.Liu, J.-F., Thorn, D.A., Zhang, Y., et al.Effects of trace amine-associated receptor 1 agonists on the expression, reconsolidation, and extinction of cocaine reward memoryInt. J. Neuropsychopharmacol.19(7)pyw009(2016)
| Cas No. | 1048346-74-2 | SDF | |
| Canonical SMILES | CCN(C1=CC=CC=C1)C[C@H]2COC(N)=N2 | ||
| Formula | C12H17N3O | M.Wt | 219.3 |
| Löslichkeit | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml | Storage | -20°C |
| 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 | 4.56 mL | 22.7998 mL | 45.5996 mL |
| 5 mM | 912 μL | 4.56 mL | 9.1199 mL |
| 10 mM | 456 μL | 2.28 mL | 4.56 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)