Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.
| Molecular Weight | 456.49 |
| Formula | C27H22F2N4O |
| CAS Number | 2172870-89-0 |
| Form | Solid |
| Solubility (25°C) | DMSO 20 mg/mL (ultrasonic and warming and heat to 60°C) |
| 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 Somatostatin Receptor Products |
|---|
| TT-232
TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. |
| Cyclosomatostatin
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. |
| Somatostatin-28 (1-14)
Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28. |
| CH 275
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. |
| CYN 154806
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist. |
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