Firazorexton hydrate (TAK-994) is a potent, brain-penetrant, and orally active orexin type 2 receptor (OX2R) agonist (EC50: 19 nM).
Molecular Weight | 497.53 |
Formula | C22H25F3N2O4S.3/2H2O |
CAS Number | 2861934-86-1 |
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.
[2] Lanyun Wang et al. ACS Omega. A Review of the Effect of Porous Media on Gas Hydrate Formation
[4] Chang Q Sun et al. Adv Colloid Interface Sci. Hydration of Hofmeister ions
[5] Tai Bui et al. J Phys Chem Lett. Antiagglomerants Affect Gas Hydrate Growth
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Orexin B, rat, mouse
Orexin B, rat, mouse (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively. |
Hypocretin (70-98), human
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Xenopus orexin A is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. |
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