| VU0152100 |
| 3-Amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide |
| (CAS 409351-28-6) |
 |
| Description： |
VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 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 with EC50 values of 1.9 ± 0.2 ?M, and increased the maximal response to ACh to approximately 130%. VU0152100 (10 ?M) also enhanced 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 (VU0152100).
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.
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| Product No. |
KT00957 |
| Product Name |
VU0152100 |
| Synonyms |
VU 0152100; VU-0152100 |
| Formal Name |
3-Amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide |
| CAS Number |
409351-28-6 |
| Molecular Formula |
C18H19N3O2S |
| Formula Weight |
341.43 |
| Formulation |
A crystalline solid |
| Purity |
98%min |
| Stability |
2 years |
| Storage |
-20°C |
| Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500 |
| Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
| Price & Availability |
In Stock. Price Negotiated. |
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