| Company Name: |
SPIRO PHARMA |
| Tel: |
|
| Email: |
eric_feng1954@126.com |
| Company Name: |
Musechem |
| Tel: |
+1-800-259-7612 |
| Email: |
info@musechem.com |
|
| | Pasireotide (for the salt) Basic information |
| Product Name: | Pasireotide (for the salt) | | Synonyms: | SOM230 L-ASPARTATE;[9-(4-aminobutyl)-3-benzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate;Pasireotide (for the salt);Pasireotide (L-aspartate salt) | | CAS: | 396091-77-3 | | MF: | C62H73N11O13 | | MW: | 1180.30892 | | EINECS: | | | Product Categories: | | | Mol File: | 396091-77-3.mol |  |
| | Pasireotide (for the salt) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 1 mg/mL (0.85 mM) | | form | Solid | | color | Off-white to light yellow |
| | Pasireotide (for the salt) Usage And Synthesis |
| Uses | Pasireotide (SOM230) L-aspartate salt, 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 L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2]. | | 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[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]. | 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 | [1] Lewis I, et, al. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem. 2003 Jun 5;46(12):2334-44. DOI:10.1021/jm021093t
[2] Quinn TJ, et, al. Pasireotide (SOM230) is effective for the treatment of pancreatic neuroendocrine tumors (PNETs) in a multiple endocrine neoplasia type 1 (MEN1) conditional knockout mouse model. Surgery. 2012 Dec;152(6):1068-77. DOI:10.1016/j.surg.2012.08.021
[3] Imhof AK, et, al. Differential antiinflammatory and antinociceptive effects of the somatostatin analogs octreotide and pasireotide in a mouse model of immune-mediated arthritis. Arthritis Rheum. 2011 Aug;63(8):2352-62. DOI:10.1002/art.30410 |
| | Pasireotide (for the salt) Preparation Products And Raw materials |
|