396091-76-2
396091-76-2
Chemical Structure
Pasireotide acetate
Synonym(s): SOM230 acetate
- CAS No.: 396091-76-2
- Formula:C60H70N10O11
- Molecular Weight:1107.26
IUPAC Name: (3S,6R,9S,12S,15S,19R,20aS)-6-((1H-indol-3-yl)methyl)-9-(4-aminobutyl)-15-benzyl-12-(4-(benzyloxy)benzyl)-1,4,7,10,13,16-hexaoxo-3-phenylicosahydropyrrolo[1,2-a][1,4,7,10,13,16]hexaazacyclooctadecin-19-yl (2-aminoethyl)carbamate acetate
InChIKey: WFKFNBBHVLMWQH-QKXVGOHISA-N
SMILES: NCCCC[C@@H](C(N[C@H]1CC2=CC=C(C=C2)OCC3=CC=CC=C3)=O)NC([C@H](NC([C@H](C4=CC=CC=C4)NC([C@H]5N(C([C@H](CC6=CC=CC=C6)NC1=O)=O)C[C@H](OC(NCCN)=O)C5)=O)=O)CC7=CNC8=C7C=CC=C8)=O.CC(O)=O
Biological Activity: Pasireotide (SOM230) acetate, 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 acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Pasireotide acetate | 99.92% | Pasireotide (SOM230) acetate, 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 acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity. | ||||||||||||||||||||
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Seglitide acetate | 98.76% | Seglitide acetate (MK-678 acetate) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide acetate also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS14, SS25 and SS28, respectively. Seglitide acetate produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide acetate inhibits glucagon secretion and reduces circulating insulin levels. Seglitide acetate causes a sustained, reversible reduction in elevated systolic blood pressure in Streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide acetate induces membrane hyperpolarization and inhibits electrical excitability. Seglitide acetate induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide acetate can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus. | ||||||||||||||||||||
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Pasireotide pamoate | 98.18% | Pasireotide (SOM230) pamoate, 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 pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity. | ||||||||||||||||||||
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Loloatin B 10 | Loloatin B 10 is an antibiotic, which exhibits antibacterial efficacy against gram positive antibiotic resistant human pathogens. | |||||||||||||||||||||
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Pasireotide | 99.94% | Pasireotide (SOM230), 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 can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. | ||||||||||||||||||||
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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. | |||||||||||||||||||||
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(2R)-Pasireotide (diaspartate) | (2R)-Pasireotide ((2R)-SOM230) diaspartate exhibits a 40-fold higher affinity for somatostatin receptor 5 than other somatostatin analogs. | |||||||||||||||||||||
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Pasireotide L-aspartate salt | 97.0% | 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. | ||||||||||||||||||||
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Veldoreotide | Veldoreotide (DG3173) a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared withOctreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent | |||||||||||||||||||||
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Veldoreotide TFA | 98.97% | Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent | ||||||||||||||||||||
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Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) | Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) is a somatostatin agonist that can be used in cancer research. | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
