Atrasentan hydrochloride (ABT-627 hydrochloride) is a potent, orally active, selective endothelin A (ETA) receptor antagonist that inhibits ETA activity and blocks endothelin-induced cellular proliferation with an IC50 value of 0.0551 nM. It can be used in studies related to prostate cancer as well as IgA nephropathy (IgAN). It can be used in prostate cancer and IgA nephropathy (IgAN) related studies.
Molecular Weight | 547.08 |
Formula | C29H38N2O6 · HCl |
CAS Number | 195733-43-8 |
Solubility (25°C) | DMSO: 2 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.
[3] Jesus Egido, et al. Atrasentan for the treatment of diabetic nephropathy
[4] A Kalliokoski, et al. Impact of OATP transporters on pharmacokinetics
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