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Pasireotide L-aspartate, formerly known as SOM230, is a potent and 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). It is an orphan drug approved for the treatment of Cushing's disease in patients who fail or are ineligible for surgical therapy. It was developed by Novartis. Pasireotide is a somatostatin analogue with a 40-fold increased affinity to somatostatin receptor 5 compared to other somatostatin analogues.
| ln Vitro |
When bound 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 demonstrates a unique high-affinity binding [1]. In primary cultures of rat pituitary cells, pasireotide L-aspartate efficiently suppresses growth hormone-releasing hormone (GHRH)-induced growth hormone (GH) production with an IC50 of 0.4 nM [1].
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| ln Vivo |
The administration of pasireotide L-aspartate (160 mg/kg/oral; subcutaneous injection for 4 months) to Pdx1-Cre resulted in significant changes in blood glucose, tumor growth, apoptosis, and serum insulin levels [2]. In a mouse model of immune-mediated arthritis, pasireotide L-aspartate (2-50 μg/kg; subcutaneously administered twice daily for 42 days) acts as an analgesic and anti-inflammatory agent via the SSTR2 receptor [3].
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| Animal Protocol |
Animal/Disease Models: 12-month-old conditional Men1 gene knockout insulinoma mice [2]
Doses: 160 mg/kg/oral Route of Administration: monthly subcutaneous injection for 4 months Experimental Results: Serum insulin diminished from 1.060 μg/L to 0.3653 μg/L, and increased blood sugar from 4.246 mM to 7.122 mM. Dramatically diminished tumor size and increased apoptosis. |
| References |
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| Molecular Formula |
C₆₂H₇₃N₁₁O₁₃
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|---|---|
| Molecular Weight |
1180.31
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| Exact Mass |
1179.538
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| CAS # |
396091-77-3
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| Related CAS # |
Pasireotide acetate;396091-76-2;Pasireotide ditrifluoroacetate;Pasireotide pamoate;396091-79-5;Pasireotide;396091-73-9;Pasireotide (diaspartate);1421446-02-7
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| PubChem CID |
78358324
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
86
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| Complexity |
2070
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| Defined Atom Stereocenter Count |
8
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| 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
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| InChi Key |
XOMKXFJQWURETI-XZRPHVMWSA-N
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| InChi Code |
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
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| Chemical 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
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| Synonyms |
SOM-230 L-aspartateSOM 230 L-aspartateSOM230 L-aspartate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~1 mg/mL (~0.85 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8472 mL | 4.2362 mL | 8.4724 mL | |
| 5 mM | 0.1694 mL | 0.8472 mL | 1.6945 mL | |
| 10 mM | 0.0847 mL | 0.4236 mL | 0.8472 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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