EPPTB (Synonyms: Ro 5212773) |
| カタログ番号GC50062 |
EPPTB (EPPTB) は、強力かつ選択的な微量アミン関連受容体 1 (TAAR1) 拮抗薬 (マウス TAAR1 の Ki = 0.9 nM) であり、他の TAAR に有意な影響はありません。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1110781-88-8
Sample solution is provided at 25 µL, 10mM.
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Trace amine 1 (TA1) receptor antagonist/inverse agonist; exhibits a higher potency at the mouse TA1 receptor than the rat and human TA1 receptors (IC50 values are 27.5, 4539 and 7487 nM, respectively). Blocks the TA1 receptor-mediated activation of an inwardly rectifying K+ current, which increases the firing frequency of dopamine (DA) neurons in the ventral tegmental area. Increases DA potency at the D2 receptor. Also displays inverse agonism, reducing basal cAMP levels in vitro (IC50 = 19 nM).
Bradaia et al (2009) The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in DArgic neurons of the mesolimbic system. Proc.Natl.Acad.Sci.U.S.A. 106 20081 PMID:19892733
| Cas No. | 1110781-88-8 | SDF | |
| 同義語 | Ro 5212773 | ||
| Canonical SMILES | O=C(NC3=CC(OCC)=CC=C3)C1=CC(C(F)(F)F)=C(N2CCCC2)C=C1 | ||
| Formula | C20H21F3N2O2 | M.Wt | 378.39 |
| 溶解度 | DMSO : 100 mg/mL (264.28 mM; Need ultrasonic) | Storage | Store at -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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6428 mL | 13.2139 mL | 26.4278 mL |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2856 mL |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 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 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.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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