| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Octreotide pamoate (SMS-201-995; Octreotide-LAR; Sandostatin, Longastatin), the pamoate salt of Octreotide, is an octapeptide and somatostatin analogue that has been approved for use in the treatment of hormone-secreting tumors; hypergastrinemia; diabetes, hypertension and small bowel fistula.
| Targets |
SSTR2/3/5
|
|---|---|
| ln Vitro |
Glycogen synthase (GS) activity is increased and phosphorylated glycogen synthase kinase 3β (GSK3β) is induced by octreotide pamoate (10–8 mM, 6 hours) [3].
|
| ln Vivo |
Subcutaneous injection of 30 mg/kg once is sufficient to greatly limit tumor growth without causing weight gain [1]. Dogs diagnosed with appendiceal osteosarcoma (OSA) can receive intramuscular injections of octreotide pamoate (60 mg/kg every 21–42 days) to reduce serum insulin-like growth factor (IGF-I) without experiencing toxicity [2]. Obese male Sprague-Dawley (SD) rats get subcutaneous injections of octreotide pamoate (40 μg/kg) every 12 hours for eight days, which improves hepatic glycogen production [3].
|
| Cell Assay |
Western Blot analysis [3]
Cell Types: Human hepatoblastoma HepG2 cell line Tested Concentrations: 10-8mM Incubation Duration: 6 hrs (hours) Experimental Results: The protein expression levels of phosphorylated Akt and GSK3β increased by 140.8% and 12.2%, respectively, and the mRNA levels increased GS has also increased. |
| Animal Protocol |
Animal/Disease Models: Female nude mice (nu/nu Balbc-A, body weight 19-22 g) [1]
Doses: 30 mg/kg Route of Administration: subcutaneous injection; primary Experimental Results: demonstrated that the average tumor volume of the treatment group was that of the control group 25.8% and had no effect on body weight. Animal/Disease Models: Dogs with appendiceal OSA [2] Doses: 60 mg/kg Route of Administration: intramuscularinjection; every 21 days; 42 days Experimental Results: Mean serum IGF-I diminished by 43% compared to mean baseline concentrations %. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (3 weeks; 40-60 g) [3] Doses: 40 μg/kg Route of Administration: subcutaneous injection; every 12 hrs (hrs (hours)); 8 days Experimental Results: Significant improvement in fat Deposit and reduce lipid penetration. |
| References |
|
| Additional Infomation |
Octreotide Pamoate is a synthetic long-acting octapeptide analogue of endogenous somatostatin. Octreotide pamoate binds to somatostatin receptors expressed by some neuroendocrine and non-neuroendocrine tumor cells, thereby initiating somatostatin receptor-mediated apoptosis. Other possible antineoplastic activities of this agent include suppression of tumor angiogenesis and tumor growth-promoting insulin-like growth factor 1 (IGF-1). (NCI04)
|
| Molecular Formula |
C72H82N10O16S2
|
|---|---|
| Molecular Weight |
1407.60889577866
|
| Exact Mass |
1396.55
|
| Elemental Analysis |
C, 61.02; H, 6.06; N, 10.02; O, 18.32; S, 4.59
|
| CAS # |
135467-16-2
|
| Related CAS # |
Octreotide;83150-76-9
|
| PubChem CID |
44194024
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0.77
|
| Hydrogen Bond Donor Count |
17
|
| Hydrogen Bond Acceptor Count |
20
|
| Rotatable Bond Count |
21
|
| Heavy Atom Count |
100
|
| Complexity |
2310
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C[C@H]([C@H]1C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)NC(=O)[C@@H](CC5=CC=CC=C5)N)C(=O)N[C@H](CO)[C@@H](C)O)O.C1=CC=C2C(=C1)C=C(C(=C2CC3=C(C(=CC4=CC=CC=C43)C(=O)O)O)O)C(=O)O
|
| InChi Key |
KFWJVABDRRDUHY-XJQYZYIXSA-N
|
| InChi Code |
InChI=1S/C49H66N10O10S2.C23H16O6/c1-28(61)39(25-60)56-48(68)41-27-71-70-26-40(57-43(63)34(51)21-30-13-5-3-6-14-30)47(67)54-37(22-31-15-7-4-8-16-31)45(65)55-38(23-32-24-52-35-18-10-9-17-33(32)35)46(66)53-36(19-11-12-20-50)44(64)59-42(29(2)62)49(69)58-41;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/h3-10,13-18,24,28-29,34,36-42,52,60-62H,11-12,19-23,25-27,50-51H2,1-2H3,(H,53,66)(H,54,67)(H,55,65)(H,56,68)(H,57,63)(H,58,69)(H,59,64);1-10,24-25H,11H2,(H,26,27)(H,28,29)/t28-,29-,34-,36+,37+,38-,39-,40+,41+,42+;/m1./s1
|
| Chemical Name |
(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide;4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid
|
| Synonyms |
SMS 201-995 pa; SMS pa; Octreotide pamoate; Octreotide pamoate; SMS 201-995 pa LAR; 135467-16-2; NSC-685403; NSC685403; DA-66304; D05230; 10-(4-aminobutyl)-19-[(2-amino-3-phenylpropanoyl)amino]-16-benzyl-N-(1,3-dihydroxybutan-2-yl)-7-(1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide;4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid;
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 0.7104 mL | 3.5521 mL | 7.1042 mL | |
| 5 mM | 0.1421 mL | 0.7104 mL | 1.4208 mL | |
| 10 mM | 0.0710 mL | 0.3552 mL | 0.7104 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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