Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. Siramesine can induce cell death in transformed cells through a mechanism including lysosomal destabilization.
In vivo, siramesine treatment of mice caused a depletion of the MC populations of the peritoneum and skin.
| Molecular Weight | 454.58 |
| Formula | C30H31FN2O |
| CAS Number | 147817-50-3 |
| Solubility (25°C) | DMSO |
| 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.
| Related Sigma Receptor Products |
|---|
| AB10
AB10 is a selective S1R antagonist. |
| WLB-89462
WLB-89462 is a selective σ2 receptor ligand (Ki: 13 nM). |
| Siramesine fumarate
Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. |
| Sigma-1 receptor antagonist 5
Sigma-1 receptor antagonist 5 and histamine H3 (hH3R, Ki=7.7 nM, IC50=215 nM). |
| AB21
AB21 is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. |
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