| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C8H10BrN |
| Purity | |
| SMILES | |
| Form | Liquid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
ZH8651 is an orally active TAAR1 agonist that activates the Gs and Gq signaling pathways. In mice, it alleviates dizocilpine-induced hyperactivity, improves prepulse inhibition deficits, and attenuates cognitive impairment. It can be used in schizophrenia research[1]. It is supplied as a colorless to light yellow liquid (C8H10BrN, MW 200.08) at 99.56% purity.
Physical & Chemical Properties
| CAS Number | 73918-56-6 |
|---|---|
| Molecular Formula | C8H10BrN |
| Molecular Weight | 200.08 g/mol |
| Purity | 99.56% |
| Appearance | Liquid |
| Color | Colorless to light yellow |
| Density | 1.29 g/cm3 |
| SMILES | BrC1=CC=C(CCN)C=C1 |
| Target | hTAAR1, mTAAR1 |
| Signaling Pathway | GPCR/G Protein |
| Solubility | In Vitro: DMSO: 100 mg/mL (499.80 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (499.80 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (12.50 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (12.50 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
ZH8651 (50 μM; 1-2 h) binds mTAAR1 in a conformation that activates both the Gs and Gq pathways[1]. ZH8651 (50 μM; 1-2 h) binds hTAAR1 in a conformation highly similar to its binding to mTAAR1, which activates the Gs pathway[1]. In transfected HEK293 cells, ZH8651 (24-48 h) acts as a dual Gs/Gq agonist at mTAAR1 and hTAAR1, with distinct residue interactions mediating activation of each pathway[1].
In Vivo
In mice, ZH8651 (0.3-3 mg/kg; p.o.; single administration; pretreatment 30 minutes before dizocilpine administration) dose-dependently attenuates schizophrenia-like hyperlocomotion, prepulse inhibition (PPI) deficits and cognitive impairment induced by dizocilpine, without reducing basal locomotor activity. At specific doses, efficacy is comparable to or better than that of SEP[1].
| Animal Model | C57BL/6J mice (male, 9-10 weeks old, Dizocilpine-induced schizophrenia-like model)[1] |
|---|---|
| Dosage | 0.3 mg/kg; 1 mg/kg; 3 mg/kg |
| Administration | p.o.; single dose; 30-minute pretreatment before dizocilpine |
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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