Pasireotide L-aspartate salt

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/ In Vitro Pasireotide 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/ In Vivo Pasireotide 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:Solid IC50& Target:pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3),

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