Ribocil is a highly selective chemical modulator of bacterial riboflavin riboswitches. Ribocil strongly inhibits GFP expression, achieving a 50% effective concentration (EC50) of 0.3 μM. Target: in vitro: Ribocil is a highly specific bioactive synthetic mimic of FMN, which competes with the natural ligand to inhibit FMN riboswitch-mediated expression of ribB and inhibits bacterial growth. Ribocil-B demonstrates superior microbiological activity as compared to Ribocil-A (minimum inhibitory concentration (MIC) = 1 μg/ml versus MIC ≥ 64 μg/ml), inhibition of riboflavin synthesis (IC50 = 0.13 μM versus IC50 > 26 μM), and binding affinity to the E. coli FMN aptamer (Kd = 6.6 nM versus Kd ≥ 10,000 nM).[1]
Molecular Weight | 382.48 |
Formula | C19H22N6OS |
CAS Number | 1381289-58-2 |
Form | Solid |
Solubility (25°C) | DMSO 12.5 mg/mL (ultrasonic) |
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.
[5] John A Howe, et al. Nature. Selective small-molecule inhibition of an RNA structural element
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