For research use only. Not for therapeutic Use.
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.
KEYWORDS: ECSI#6 | SERT inhibitor | CAS [860456-56-0] | Serotonin |SERT | Inhibitor | Proteins
| Catalog Number | I047704 |
| CAS Number | 860456-56-0 |
| Molecular Formula | C18H17NO5 |
| Purity | ≥95% |
| IUPAC Name | N-[1,3-bis(1,3-benzodioxol-5-yl)propan-2-yl]formamide |
| 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) |
| SMILES | C1OC2=C(O1)C=C(C=C2)CC(CC3=CC4=C(C=C3)OCO4)NC=O |
| Reference | S Bhat et al. A mechanism of uncompetitive inhibition of the serotonin transporter. Elife. 2023 Jan 17;12:e82641. |
