Pasireotide L-aspartate salt (C09-1165-035)

Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5 , pK i =8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activityIn VitroPasireotide L-aspartate salt exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pK i =8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC 50 of 0.4 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoPasireotide L-aspartate salt (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre. Pasireotide L-aspartate salt (2-50 μg/kg; s.c. twice daily for 42 days) exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 12 month-old conditional Men1 knockout mice with insulinomaDosage: 160 mg/kg/mouth Administration: S.c. every month for 4 months Result: Decreased the serum insulin from 1.060 μg/L to 0.3653 μg/L and increased the serum glucose from 4.246 mM to 7.122 mM. Significantly reduced the tumor size and increased apoptosis.Form:SolidIC50& Target:pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5). Specifications and Purity: ≥98.0%. Molecular Formula: C62H73N11O13. Molecular Weight: 1180.31.