| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
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| Other Sizes |
| Targets |
Trace amine-associated receptor 1 (TAAR1). ZH8651 functions as a TAAR1 agonist, capable of activating both Gs and Gq signaling pathways downstream of the receptor. This leads to an increase in intracellular cAMP and calcium flux.
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|---|---|
| ln Vitro |
ZH8651 is an agonist of TAAR1 and can activate both Gs and Gq signaling pathways. This suggests it can trigger multiple distinct cellular responses downstream of TAAR1 activation, making it a useful tool for studying the receptor's full pharmacological profile. No specific in vivo activity data is reported, but the compound is noted for its potential in schizophrenia research.
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| ln Vivo |
Given its ability to cross the blood-brain barrier (as a small, lipophilic amine), ZH8651 is used in vivo to investigate the role of TAAR1 in modulating dopaminergic and glutamatergic systems. It is thought to mimic the effects of endogenous TAAR1 agonists and is therefore utilized in studies of schizophrenia and other psychiatric disorders.
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| Enzyme Assay |
A cell-free binding assay for TAAR1 can be performed using membrane preparations from cells expressing the receptor. Membranes are incubated with a radiolabeled TAAR1 antagonist (e.g., [3H]EPPTB) and varying concentrations of unlabeled ZH8651. After incubation, bound and free ligand are separated by filtration, and radioactivity is counted to determine the compound's affinity (Ki).
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| Cell Assay |
A cellular cAMP assay is standard. HEK293 cells stably expressing TAAR1 are seeded in 96-well plates. After serum starvation, cells are treated with varying concentrations of ZH8651. Intracellular cAMP levels are measured using a HTRF or chemiluminescence-based detection kit to determine the agonist's EC50 and efficacy. Calcium flux assays can also be performed to assess Gq pathway activation.
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| Animal Protocol |
In vivo studies in rodent models of schizophrenia are used. ZH8651 can be administered intraperitoneally (i.p.) in a suitable vehicle. Behavior is assessed using tests such as prepulse inhibition (PPI) of the startle response and locomotor activity. The compound's effects on dopamine and glutamate levels in specific brain regions can also be measured by microdialysis.
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| ADME/Pharmacokinetics |
Not reported. As a small molecule agonist, it is expected to have some degree of oral bioavailability, but its PK profile has not been formally characterized. Based on its structure, metabolism likely involves deamination and conjugation pathways.
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| Toxicity/Toxicokinetics |
Not reported. Given that ZH8651 is a substituted phenylethylamine, it may share some pharmacological properties with other amines, and high doses could potentially lead to sympathomimetic-like effects. As a research tool, no formal toxicology data is available.
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| References | |
| Additional Infomation |
ZH8651 is a key tool for understanding TAAR1's unique mechanism as an intracellular receptor that can be activated by both endogenous and exogenous amines. Its ability to activate both Gs and Gq pathways distinguishes it from other TAAR1 agonists that may be biased toward a single pathway. This makes it valuable for studying the complex, context-dependent signaling of TAAR1 in its native environment, particularly in the brain's reward and emotional circuits.
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| Molecular Formula |
C8H10BRN
|
|---|---|
| Molecular Weight |
200.08
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| Exact Mass |
198.999
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| CAS # |
73918-56-6
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| PubChem CID |
533915
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
271.3±0.0 °C at 760 mmHg
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| Flash Point |
113.1±20.4 °C
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| Vapour Pressure |
0.0±0.5 mmHg at 25°C
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| Index of Refraction |
1.576
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| LogP |
2.23
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
10
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| Complexity |
87.3
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
BrC1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])N([H])[H]
|
| InChi Key |
ZSZCXAOQVBEPME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H10BrN/c9-8-3-1-7(2-4-8)5-6-10/h1-4H,5-6,10H2
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| Chemical Name |
2-(4-bromophenyl)ethanamine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~499.8 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9980 mL | 24.9900 mL | 49.9800 mL | |
| 5 mM | 0.9996 mL | 4.9980 mL | 9.9960 mL | |
| 10 mM | 0.4998 mL | 2.4990 mL | 4.9980 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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