Pasireotide L-aspartate salt

• CAT Number: I003447
• CAS Number: 396091-77-3
• Molecular Formula: C62H73N11O13
• Molecular Weight: 1180.33
• Purity: ≥95%
• Target: Neuronal Signaling
• Solubility: 10 mM in DMSO
• Storage: Store at -20C
• IC50: 8.2/9.0/9.1/<7.0/9.9(pKi, sst1/2/3/4/5) [1]
• IUPAC Name: (2S)-2-aminobutanedioic acid;[(3S,6S,9S,12R,15S,18S,20R)-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
• InChI: InChI=1S/C58H66N10O9.C4H7NO4/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45;5-2(4(8)9)1-3(6)7/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72);2H,1,5H2,(H,6,7)(H,8,9)/t43-,46+,47+,48-,49+,50+,51+;2-/m10/s1
• InChIKey: XOMKXFJQWURETI-XZRPHVMWSA-N
• SMILES: C1[C@H](CN2[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](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@@H](C(=O)O)N)C(=O)O

Pasireotide L-aspartate salt（Cat No.:I003447）is a synthetic compound used in the treatment of certain endocrine disorders, particularly Cushing’s disease and acromegaly. It is a long-acting somatostatin analog that binds to and activates somatostatin receptors, inhibiting the release of growth hormone (GH) and cortisol. By reducing the secretion of these hormones, pasireotide helps control abnormal hormone levels in patients with pituitary tumors. The L-aspartate salt form enhances its solubility and bioavailability, enabling prolonged therapeutic effects. It is administered via injection and is typically used when other treatments are ineffective or not suitable.

Reference

[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.
[2]. Hofland LJ, et al. The novel somatostatin analog SOM230 is a potent inhibitor of hormone release by growth hormone- and prolactin-secreting pituitary adenomas in vitro. J Clin Endocrinol Metab. 2004 Apr;89(4):1577-85.
[3]. Murray RD, et al. The novel somatostatin ligand (SOM230) regulates human and rat anterior pituitary hormone secretion. J Clin Endocrinol Metab. 2004 Jun;89(6):3027-32.
[4]. 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.
[5]. 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.