Pasireotide |
Catalog No.GC10729
One-Click Copy Product Info
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Pasireotide (SOM230), un anÁlogo de somatostatina de ciclohexapéptido de acciÓn prolongada, puede mejorar la actividad agonista en los receptores de somatostatina (subtipos sst1/2/3/4/5, pKi = 8.2/9.0/9.1/<7.0/9.9, respectivamente).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 396091-73-9
Sample solution is provided at 25 µL, 10mM.
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Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that 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).IC50 value: 8.2/9.0/9.1/<7.0/9.9(pKi, sst1/2/3/4/5) [1]in vitro: SOM230 showed a lower potency of GH release inhibition (IC(50), 0.5 nM), compared with OCT (IC(50), 0.02 nM) and SRIF-14 (IC(50), 0.02 nM). A positive correlation was found between sst(2) but not sst(5) mRNA levels in the adenoma cells and the inhibitory potency of OCT on GH release in vivo and in vitro, and the effects of SOM230 and SRIF-14 in vitro [2]. In cultures of human fetal pituitary cells, SOM230 inhibited GH secretion by 42 +/- 9% (P = 0.002) but had no effect on TSH release. SOM230 inhibited GH release from GH-secreting adenoma cultures by 34 +/- 8% (P = 0.002), PRL by 35 +/- 4% from PRL-secreting adenomas (P = 0.01), and alpha-subunit secretion from nonfunctioning pituitary adenomas by 46 +/- 18% (P = 0.34) [3].in vivo: On day 7, there was a decrease in serum insulin levels from 1.06 ± 0.28 μg/L to 0.37 ± 0.17 μg/L (P = .0128) and a significant increase in serum glucose from 4.2 ± 0.45 mmol/L to 7.12 ± 1.06 mmol/L (P = .0075) in the treatment group but no change in the control group [4]. In wild-type mice, both octreotide and pasireotide significantly attenuated knee joint swelling and histopathologic manifestations of arthritis to an extent comparable to that of dexamethasone. In SSTR2(-/-) mice, the antiinflammatory effects of both octreotide and pasireotide were completely abrogated [5].
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.
[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.
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Animal experiment: |
Mice are anesthetized using halothane and then shaved on their flank for subcutaneous injection of either phosphate buffered saline (PBS) buffer or Pasireotide at a concentration of 160 mg/Kg/month (64 mg/mL) every month for 4 months. The mice underwent a 24-h fast prior to collecting whole blood via a retro-orbital bleeding technique weekly at pre- and post-treatments. Serum glucose is measured by enzymatic colorimetric assay using a GM7 Analyzer. Serum insulin is measured by enzyme-linked immunosorbent assay (ELISA) with the UltrasensitiveMouse Insulin ELISA kit according to the manufacturer’s instructions. |
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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. |
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| Cas No. | 396091-73-9 | SDF | |
| Chemical Name | (E)-(1Z,3S,4Z,6R,7Z,9S,10Z,12S,13Z,15S,19R,20aS)-6-((1H-indol-3-yl)methyl)-9-(4-aminobutyl)-15-benzyl-12-(4-(benzyloxy)benzyl)-1,4,7,10,13-pentahydroxy-16-oxo-3-phenyl-3,6,9,12,15,16,18,19,20,20a-decahydropyrrolo[1,2-a][1,4,7,10,13,16]hexaazacyclooctadeci | ||
| Canonical SMILES | NCCCC[C@@](/N=C(O)/[C@@](/N=C(O)/[C@](/N=C(O)/[C@]1([H])C[C@](O/C(O)=N/CCN)([H])CN12)([H])C3=CC=CC=C3)([H])CC4=CNC5=CC=CC=C45)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](C2=O)([H])CC6=CC=CC=C6)([H])CC7=CC=C(OCC8=CC=CC=C8)C=C7 | ||
| Formula | C58H66N10O9 | M.Wt | 1047.21 |
| Solubility | Soluble in water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 954.9 μL | 4.7746 mL | 9.5492 mL |
| 5 mM | 191 μL | 954.9 μL | 1.9098 mL |
| 10 mM | 95.5 μL | 477.5 μL | 954.9 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)