Bryostatin 1 is a natural macrolide isolated from the moss bug Bugula neritina and a potent PKC modulator of central nervous system (CNS) permeability.Bryostatin 1 binds to the isolated Munc13-1 C1 domain and the full-length Munc13-1 protein with a Ki value of 8.07 and 0.45 nM, respectively, and has anticancer, anti-inflammatory and neuroprotective activities. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Ki values of 8.07 nM and 0.45 nM, respectively, and exhibits anticancer, anti-inflammatory, and neuroprotective activities.
Molecular Weight | 905.03 |
Formula | C47H68O17 |
CAS Number | 83314-01-6 |
Form | Solid |
Solubility (25°C) | DMSO: soluble |
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] Michael D Kornberg, et al. Bryostatin-1 alleviates experimental multiple sclerosis
[4] Miao-Kun Sun, et al. Bryostatin-1: pharmacology and therapeutic potential as a CNS drug
[5] Jeremy Kortmansky, et al. Bryostatin-1: a novel PKC inhibitor in clinical development
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