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Pasireotide L-aspartate salt
CAS No. 396091-77-3
Pasireotide L-aspartate salt( SOM230 L-aspartate )
Catalog No. M14363 CAS No. 396091-77-3
A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 10MG | 822 | Get Quote |
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| 100MG | Get Quote | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NamePasireotide L-aspartate salt
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors.
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DescriptionA potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively); effectively inhibits GHRH-induced growth hormone release in primary cultures of rat pituitary cells with IC50 of 0.4 nM, also potently suppresses GH secretion in rats.Cushing's Disease Approved.
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In VitroPasireotide L-aspartate salt 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).Pasireotide L-aspartate salt 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.
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In VivoPasireotide 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.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. Animal Model:12 month-old conditional Men1 knockout mice with insulinoma 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.
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SynonymsSOM230 L-aspartate
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PathwayGPCR/G Protein
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TargetSomatostatin Receptor
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RecptorSomatostatin Receptor
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Research AreaEndocrinology
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IndicationCushing Disease
Chemical Information
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CAS Number396091-77-3
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Formula Weight1180.309
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Molecular FormulaC62H73N11O13
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESC1C(CN2C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(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(C(=O)O)N)C(=O)O
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Chemical NameCyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl], L-aspartate (1:x)
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Lewis I, et al. J Med Chem. 2003 Jun 5;46(12):2334-44.
2. Bruns C, et al. Eur J Endocrinol. 2002 May;146(5):707-16.
3. Hofland LJ, et al. Eur J Endocrinol. 2005 Apr;152(4):645-54.
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