Entacapone is an inhibitor of FTO demethylation with IC50 of 3.5 μM, Entacapone also inhibits catechol-O-methyltransferase (COMT) with IC50 of 151 nM.
| Molecular Weight | 305.29 |
| Formula | C14H15N3O5 |
| CAS Number | 130929-57-6 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FTO Products |
|---|
| ZLD115
ZLD115 is a FB23-derivated inhibitor of Fat Mass and Obesity-associated Protein (FTO). |
| Meclofenamic acid sodium hydrate
Meclofenamic acid sodium hydrate is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid sodium hydrate inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively. |
| Meclofenamic acid
Meclofenamic acid (Meclofenamate) is a non-steroidal anti-inflammatory agent. Meclofenamic acid is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker. Meclofenamic acid inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively. |
| FB23
FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity. |
| Dac51
Dac51 is an effective FTO inhibitor with an IC50 of 0.4 μM against FTO demethylation. |
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