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ECSI#6
- Soluble in DMSO and EtOH
- MF: C18H17NO5
- MW: 327.33
Description
ECSI#6 is the first uncompetitive serotonin transporter (SERT) inhibitor. Inhibition of serotonin uptake by ECSI#6 was enhanced with increasing serotonin concentration. Conversely, the KM for serotonin was lowered by augmenting ECSI#6. ECSI#6 bound with low affinity to the outward-facing state of SERT but with increased affinity to a potassium-bound state. ECSI#6 also acted as a pharmacochaperone: cellular preincubation with ECSI#6 restored export from the endoplasmic reticulum (ER) and substrate transport by a misfolded SERT variant.
More Information
| Parent CAS No. | 860456-56-0 |
|---|---|
| Chemical Name | N-(1,3-Di(benzo[d][1,3]dioxol-5-yl)propan-2-yl)formamide |
| SMILES | C12OCOC=1C=CC(CC(NC=O)CC1C=CC3OCOC=3C=1)=C2 |
| MFCD | N.A. |
| InChi | InChI=1S/C18H17NO5/c20-9-19-14(5-12-1-3-15-17(7-12)23-10-21-15)6-13-2-4-16-18(8-13)24-11-22-16/h1-4,7-9,14H,5-6,10-11H2,(H,19,20) |
| InChiKey | HNEITUUMXZICIV-UHFFFAOYSA-N |
| CID | 53325404 |
| Short Description | SERT inhibitor |
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