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VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $34 | In Stock | |
| 5 mg | $81 | In Stock | |
| 10 mg | $121 | In Stock | |
| 25 mg | $267 | In Stock | |
| 50 mg | $428 | In Stock | |
| 100 mg | $645 | In Stock | |
| 200 mg | $887 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $100 | In Stock |
| Description | VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM). |
| In vitro | VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh (EC50: 1.9 ± 0.2 μM) and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also increased the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM [1]. |
| In vivo | Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval [1]. |
| Synonyms | VU152100 |
| Molecular Weight | 341.43 |
| Formula | C18H19N3O2S |
| Cas No. | 409351-28-6 |
| Smiles | COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1 |
| Relative Density. | 1.282 g/cm3 |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (161.09 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.86 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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