TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.
| Molecular Weight | 561.26 |
| CAS Number | 500794-88-7 |
| Solubility (25°C) | DMSO ≥ 83.3 mg/mL |
| Storage | 2-8°C, protect from light |
| 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] Giulia Iannaccone, et al. Weathering the Cytokine Storm in COVID-19: Therapeutic Implications
[2] Miao Miao, et al. Clinical significance of chemokine receptor antagonists
[5] Cihat Safak, et al. Fused 1,4-dihydropyridines as potential calcium modulatory compounds
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