ZH8651
Based on 1 Customer Validation
ZH8651 is an orally active TAAR1 agonist. ZH8651 activates the Gs and Gq signaling pathways. ZH8651 alleviates dizocilpine-induced hyperactivity, improves prepulse inhibition deficits, and attenuates cognitive impairment in mice. ZH8651 can be used for the research of schizophrenia.
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- Pureté: 99.56%
- CAS No.: 73918-56-6
- Formule: C8H10BrN
- Masse moléculaire:200.08
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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hTAAR1 |
mTAAR1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
1540 nM
Compound: 10
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Agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization by calcium 3 assay
Agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization by calcium 3 assay
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[PMID: 18602830] |
ZH8651 (50 μM; 1-2 h) binds to mTAAR1 in a conformation that activates the Gs and Gq pathways[1].
ZH8651 (50 μM; 1-2 h) binds to hTAAR1 in a conformation highly similar to that of its mTAAR1 binding, thereby activating the Gs pathway[1].
ZH8651 (24-48 h) acts as a dual Gs/Gq agonist for mTAAR1 and hTAAR1 in transfected HEK293 cells, with distinct residue interactions mediating the activation of each pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 0.18 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, 9-10 weeks old, Dizocilpine-induced schizophrenia-like model)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; single dose; 30-minute pretreatment before dizocilpine
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Result:Dose-dependently inhibited Dizocilpine-induced hyperlocomotion, with efficacy similar to SEP and no reduction of baseline locomotion at any dose.
Dose-dependently improved Dizocilpine-induced PPI reduction; at 1 mg/kg, showed a stronger effect than SEP at the same dose for the 82-120 dB prepulse intensity; at 3 mg/kg, showed a stronger effect than SEP at the same dose for 78-120 dB and 82-120 dB prepulse intensities.
Significantly attenuated Dizocilpine-induced cognitive deficits in the NOR test at 3 mg/kg, with efficacy comparable to SEP at the same dose.
Greatly diminished beneficial effects on schizophrenia-like phenotypes in Taar1-/- mice.
Chemical Information
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CAS No. 73918-56-6
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Appearance Liquid (Density: 1.29 g/cm3)
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Masse moléculaire 200.08
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Formule C8H10BrN
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Color Colorless to light yellow
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SMILES
BrC1=CC=C(CCN)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : 100 mg/mL (499.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Korean - KR (476 KB)
- Portuguese - PT (476 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.9980 mL | 24.9900 mL | 49.9800 mL | 124.9500 mL |
| 5 mM | 0.9996 mL | 4.9980 mL | 9.9960 mL | 24.9900 mL | |
| 10 mM | 0.4998 mL | 2.4990 mL | 4.9980 mL | 12.4950 mL | |
| 15 mM | 0.3332 mL | 1.6660 mL | 3.3320 mL | 8.3300 mL | |
| 20 mM | 0.2499 mL | 1.2495 mL | 2.4990 mL | 6.2475 mL | |
| 25 mM | 0.1999 mL | 0.9996 mL | 1.9992 mL | 4.9980 mL | |
| 30 mM | 0.1666 mL | 0.8330 mL | 1.6660 mL | 4.1650 mL | |
| 40 mM | 0.1250 mL | 0.6248 mL | 1.2495 mL | 3.1238 mL | |
| 50 mM | 0.1000 mL | 0.4998 mL | 0.9996 mL | 2.4990 mL | |
| 60 mM | 0.0833 mL | 0.4165 mL | 0.8330 mL | 2.0825 mL | |
| 80 mM | 0.0625 mL | 0.3124 mL | 0.6248 mL | 1.5619 mL | |
| 100 mM | 0.0500 mL | 0.2499 mL | 0.4998 mL | 1.2495 mL |
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