FTO-IN-17
Based on 1 Customer Validation
FTO-IN-17 is an orally active and brain-penetrant FTO (m6A RNA demethylase) inhibitor with an IC50 of 1.1 μM. FTO-IN-17 stably binds the FTO catalytic pocket. FTO-IN-17 protects against Aβ1-42-induced toxicity while increasing global m6A levels and dampening pro-inflammatory gene (CXCL10, TNF-α) expression. FTO-IN-17 ameliorates anxiety-like behavior and rescues hippocampal-dependent spatial, recognition memory and neuroinflammation in Alzheimer's disease mice models.
For research use only. We do not sell to patients.
- Purity : 99.38%
- CAS No.: 1434867-98-7
- Formula: C20H23FN4O2
- Molecular Weight:370.42
-
Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
In Vitro
FTO-IN-17 (Compound VI) exhibits high in vitro blood-brain barrier permeability (Pe = 12.2 × 10-6 cm/s)[1].
FTO-IN-17 (0.01-50 μM; overnight) potently inhibits human FTO demethylase activity with an IC50 of 1.1 μM[1].
FTO-IN-17 (10 μM; overnight) is fully selective for human FTO over human ALKBH5 demethylase, showing no inhibition of ALKBH5 at 10 μM[1].
The (S)-stereoisomer of FTO-IN-17 exhibits significantly stronger, more stable binding to human FTO than the (R)-stereoisomer, with over 7 times higher calculated binding affinity[1].
FTO-IN-17 (0.001-50 μM; 30 min pre-incubation + 24 h co-incubation) provides sustained, dose-dependent neuroprotection against Aβ1-42-induced toxicity in differentiated SH-SY5Y cells, increases global m6A levels, and downregulates pro-inflammatory gene expression at 1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:differentiated SH-SY5Y human neuroblastoma cells
-
Concentration:0.001, 0.01, 0.1, 1, 10, 50 μM
-
Incubation Time:30 min pre-incubation, followed by 24 h co-incubation with 5 μM Aβ1-42
-
Result:Demonstrated dose-dependent neuroprotection, with 70-85% cell viability at 0.1-10 μM.
Significantly increased global m6A RNA methylation levels compared to Aβ1-42-treated cells at 1 μM.
Significantly downregulated mRNA expression of pro-inflammatory genes CXCL10, TNF-α, and HMOX1 at 1 μM.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | Cmax (Brain) | Tmax (Brain) | Brain-Kp |
|---|---|---|---|---|---|---|---|
| Mice[1] | 3 mg/kg | p.o. | 51.3 ng/mL | 5 min | 29.9 ng/g | 5 min | 58 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Alzheimer's disease model (SAMP8, 5-month-old female; sporadic Alzheimer's disease model)[1]
-
Dosage:3 mg/kg
-
Administration:p.o.; daily; 28 days
-
Result:Significantly reduced anxiety-like behavior via decreased rearing and grooming in the open field test.
Rescued hippocampal-dependent spatial memory, with object location test discrimination index recovered to levels comparable to SAMR1 control mice.
Significantly increased both short-term and long-term recognition memory relative to SAMP8 control mice via novel object recognition test discrimination indices.
Increased global m6A methylation levels in brain tissue.
Upregulated expression of synaptic plasticity genes Arc and Egr1 in brain tissue.
Downregulated expression of neuroinflammatory genes Cxcl10, iNOS, and Hmox1 in brain tissue.
Chemical Information
-
CAS No. 1434867-98-7
-
Appearance Solid
-
Molecular Weight 370.42
-
Formula C20H23FN4O2
-
Color Light yellow to yellow
-
SMILES
CC(C1=NOC(C2CCCN(C2)CC3=NC4=C(C=CC=C4C(O)=C3)F)=N1)C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (67.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6996 mL | 13.4982 mL | 26.9964 mL | 67.4910 mL |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL | 13.4982 mL | |
| 10 mM | 0.2700 mL | 1.3498 mL | 2.6996 mL | 6.7491 mL | |
| 15 mM | 0.1800 mL | 0.8999 mL | 1.7998 mL | 4.4994 mL | |
| 20 mM | 0.1350 mL | 0.6749 mL | 1.3498 mL | 3.3745 mL | |
| 25 mM | 0.1080 mL | 0.5399 mL | 1.0799 mL | 2.6996 mL | |
| 30 mM | 0.0900 mL | 0.4499 mL | 0.8999 mL | 2.2497 mL | |
| 40 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.6873 mL | |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5399 mL | 1.3498 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL |
FTO-IN-17 Related Classifications
HY-183325 Related Classifications
Powered by Bioz