Hexaminolevulinate (HAL) hydrochloride is a hexyl ester of 5-Aminolevulinic acid (ALA), a precursor to porphyrins including the photosensitizer protoporphyrin IX (PPIX). Hexaminolevulinate is more lipophilic than ALA, and is 50–100 times more efficient than ALA at inducing PpIX, which accumulates preferentially in neoplastic cells. Hexaminolevulinate administration followed by light activation has been used for fluorescence cystoscopy to enhance detection of bladder cancer, in particular carcinoma in situ (CIS). Hexaminolevulinate is also being studied for use in cancer photodynamic therapy. Hexaminolevulinate followed by irradiation produced DNA oxidative damage and apoptosis.
| Molecular Weight | 251.75 |
| Formula | C11H21NO3 · HCl |
| CAS Number | 140898-91-5 |
| Solubility (25°C) | Water: 20 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.
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