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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 | |
2 mg | $48 | In Stock | |
5 mg | $81 | In Stock | |
10 mg | $121 | In Stock | |
25 mg | $267 | In Stock | |
50 mg | $519 | In Stock | |
100 mg | $779 | In Stock | |
200 mg | $1,090 | In Stock | |
500 mg | $1,650 | 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]. |
Alias | VU152100 |
Molecular Weight | 341.43 |
Formula | C18H19N3O2S |
Cas No. | 409351-28-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (161.09 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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