| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Purity: ≥98%
Pasireotide pamoate (formerly SOM-230; SOM230) is the pamoate salt of Pasireotide, which is a cyclohexapeptide somatostatin mimic and 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 |
The human somatostatin receptor (subtypes sst1/2/3/4/5, pKi 8.2/9.0/9.1/<7.0/9.9, respectively) reacts uniquely and highly favorably to pasireotide pamoate[1]. With an effective inhibitory concentration (IC50 of 0.4 nM), pasireotide pamoate suppresses growth hormone-releasing hormone (GHRH)-induced growth hormone (GH) release in primary cultures of rat pituitary cells.
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|---|---|
| ln Vivo |
Pasireotide pamoate (160 mg/kg/oral; subcutaneous injection for 4 months) dramatically lowered serum insulin, raised blood glucose, reduced tumor growth, and enhanced apoptosis in Pdx1-Cre [2]. Pasireotide pamoate (2-50 μg/kg; subcutaneously administered twice daily for 42 days) produces analgesic and anti-inflammatory effects through the SSTR2 receptor in a mouse model of immune-mediated arthritis [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. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation The excretion of pasireotide into breastmilk has not been studied. However, because it has a high molecular weight of 1047 daltons it is likely to be poorly excreted into breastmilk and it is a peptide that is likely digested in the infant's gastrointestinal tract. It is unlikely to reach the clinically important levels in infant serum. However, the manufacturer states that nursing mothers should not use pasireotide. An alternate drug is preferred. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
See also: Pasireotide (has active moiety).
|
| Molecular Weight |
1435.57580041885
|
|---|---|
| Exact Mass |
1434.596
|
| CAS # |
396091-79-5
|
| Related CAS # |
Pasireotide acetate;396091-76-2;Pasireotide ditrifluoroacetate;Pasireotide L-aspartate salt;396091-77-3;Pasireotide;396091-73-9;Pasireotide (diaspartate);1421446-02-7
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| PubChem CID |
11982961
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
13
|
| Hydrogen Bond Acceptor Count |
17
|
| Rotatable Bond Count |
22
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| Heavy Atom Count |
106
|
| Complexity |
2510
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| Defined Atom Stereocenter Count |
7
|
| SMILES |
O(C(NCCN)=O)[C@H]1CN2C([C@H](CC3C=CC=CC=3)NC([C@H](CC3C=CC(=CC=3)OCC3C=CC=CC=3)NC([C@H](CCCCN)NC([C@@H](CC3=CNC4C=CC=CC3=4)NC([C@H](C3C=CC=CC=3)NC([C@@H]2C1)=O)=O)=O)=O)=O)=O.OC1C(C(=O)O)=CC2C=CC=CC=2C=1CC1=C(C(C(=O)O)=CC2C=CC=CC1=2)O
|
| InChi Key |
HSXBEUMRBMAVDP-QKXVGOHISA-N
|
| InChi Code |
InChI=1S/C58H66N10O9.C23H16O6/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;24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29/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);1-10,24-25H,11H2,(H,26,27)(H,28,29)/t43-,46+,47+,48-,49+,50+,51+;/m1./s1
|
| Chemical 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 4,4'-methylenebis(3-hydroxy-2-naphthalenecarboxylate)
|
| Synonyms |
Pasireotide pamoate; SOM 230; SOM230; SOM-230; trade name: Signifor; Signifor LAR.
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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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.6966 mL | 3.4829 mL | 6.9658 mL | |
| 5 mM | 0.1393 mL | 0.6966 mL | 1.3932 mL | |
| 10 mM | 0.0697 mL | 0.3483 mL | 0.6966 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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