Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity atsomatostatin receptors(subtypessst1/2/3/4/5,pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity^[1][2].

pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3),<7.0 (sst4), 9.9 (sst5)^[1]

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/<7.0/9.9, respectively)^[1].
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 IC₅₀of 0.4 nM^[1].

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 inPdx1-Cre^[2].
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^[3].

1180.31

Solid

C₆₂H₇₃N₁₁O₁₃

396091-77-3

帕瑞肽天门冬氨酸盐

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 1 mg/mL(0.85 mM;Need ultrasonic)