AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
| Molecular Weight | 583.58 |
| Formula | C25H28F3N5O6S |
| CAS Number | 1314217-69-0 |
| Form | Solid |
| Solubility (25°C) | DMSO 41.67 mg/mL (ultrasonic) |
| Storage | 4°C, dry, sealed |
| 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.
[1] Yoshiharu Uno. Intern Emerg Med. Camostat mesilate therapy for COVID-19
[2] Ferdi Schüth. Science. Making more from methane
[4] Sarika Jain, et al. Clin Cancer Res. Eribulin mesylate
[5] Timothy K Huyck, et al. Nat Rev Drug Discov. Eribulin mesylate
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