Pasireotide L-aspartate salt

Research use only, not for human use.

A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors.

A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively); effectively inhibits GHRH-induced growth hormone release in primary cultures of rat pituitary cells with IC50 of 0.4 nM, also potently suppresses GH secretion in rats.Cushing's Disease Approved.

Pasireotide L-aspartate salt exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=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 IC50 of 0.4 nM.

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. Animal Model:12 month-old conditional Men1 knockout mice with insulinoma Dosage: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.

SOM230 L-aspartate

GPCR/G Protein

Somatostatin Receptor

Somatostatin Receptor

Endocrinology

Cushing Disease

396091-77-3

1180.309

C62H73N11O13

>98% (HPLC)

10 mM in DMSO

C1C(CN2C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C2=O)CC3=CC=CC=C3)CC4=CC=C(C=C4)OCC5=CC=CC=C5)CCCCN)CC6=CNC7=CC=CC=C76)C8=CC=CC=C8)OC(=O)NCCN.C(C(C(=O)O)N)C(=O)O

Cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl], L-aspartate (1:x)

(-20℃)

With Ice Pack

≥ 2 years