Pasireotide (diaspartate)
Modify Date: 2024-01-06 12:49:46
Pasireotide (diaspartate) structure
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Common Name | Pasireotide (diaspartate) | ||
|---|---|---|---|---|
| CAS Number | 1421446-02-7 | Molecular Weight | 1313.41 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C66H80N12O17 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Pasireotide (diaspartate)Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2]. |
| Name | Pasireotide (diaspartate) |
|---|
| Description | Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2]. |
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| Related Catalog | |
| Target |
pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1] |
| In Vitro | Pasireotide diaspartate 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)[1]. Pasireotide diaspartate 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[1]. |
| In Vivo | Pasireotide (160 mg/kg/mouth; s.c. for 4 months) diaspartate significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre[2]. Pasireotide (2-50 μg/kg; s.c. twice daily for 42 days) diaspartate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis[3]. Animal Model: 12 month-old conditional Men1 knockout mice with insulinoma[2] 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. |
| References |
| Molecular Formula | C66H80N12O17 |
|---|---|
| Molecular Weight | 1313.41 |