C75 trans is an enantiomer of C75, which is a synthetic fatty-acid synthase (FASN) inhibitor. trans-C75 ((±)-C75) inhibits PC3 cell growht with an IC50 of 35 μM at 24 h. trans-C75 ((±)-C75)(10-50 μM) also reduces the growth of LNCaP spheroids in a concentration-dependent manner with an IC50 of 50 μM.
In vivo, intraperitoneal administration of C75 at 30 mg/kg body weight inhibits food intake of mice by ≥95% within 2 h after i.p. injection. C75 treatment of rodent adipocytes and hepatocytes and human breast cancer cells increases fatty acid oxidation and ATP levels by increasing CPT-1 activity, even in the presence of elevated concentrations of malonyl-CoA.
| Molecular Weight | 254.32 |
| Formula | C14H22O4 |
| CAS Number | 191282-48-1 |
| Solubility (25°C) | DMSO ≥ 25 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.
[5] J Ofengand, et al. Pseudouridines and pseudouridine synthases of the ribosome
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