(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48). (S)-(+)-Dimethindene maleate (2 μM; 1 h) significantly impaires the developmental potency of mouse extended pluripotent stem (mEPS) cells in chimeric blastocysts and leads to rapid differentiation of primed human pluripotent stem cell (hPSC)-converted hEPS cells.
Molecular Weight | 408.49 |
Formula | C24H28N2O4 |
CAS Number | 136152-65-3 |
Solubility (25°C) | DMSO 90 mg/mL |
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.
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