Pasireotide is a somatostatin analog with a 40-fold increased affinity to somatostatin receptor 5 compared to other somatostatin analogs. Pasireotide (SOM 230) exhibits unique high-affinity binding to human somatostatin receptors sst1/2/3/4/5 with pKi of 8.2/9.0/9.1/<7.0/9.9 respectively. In cultures of human fetal pituitary cells, SOM230 inhibited GH secretion by 42 +/- 9% (P = 0.002) but had no effect on TSH release. SOM230 inhibited GH release from GH-secreting adenoma cultures by 34 +/- 8% (P = 0.002), PRL by 35 +/- 4% from PRL-secreting adenomas (P = 0.01), and alpha-subunit secretion from nonfunctioning pituitary adenomas by 46 +/- 18% (P = 0.34).
| Molecular Weight | 1047.21 |
| Formula | C58H66N10O9 |
| CAS Number | 396091-73-9 |
| 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 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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