| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Octreotide acetate (SMS201-995; Sandostatin, SMS201995; Samilstin; Sandostatina; Octreotide-LAR; Longastatin), the acetate salt of Octreotide, is an octapeptide and somatostatin analogue acting as an agonist for sst2, sst3 and sst5 somatostatin receptors. It is approved to treat small bowel fistula, diabetes, hypertension, hypergastrinemia, and hormone-secreting tumors.
| ln Vitro |
Octreotide-treated groups demonstrate a substantially lower tumor volume in comparison to the saline group. Greater antitumor effect is shown by Octreotide-PPSG (1.4 mg/kg, i.p.) compared to Octreotide-soln (100 μg/kg, i.p.). When comparing the saline group to the primary HCC-bearing rats, octreotide treatments significantly inhibit the expression levels of SSTR2 and SSTR5. The results indicate that the Octreotide-PPSG group appears to inhibit SSTR2 and SSTR5 expression more than the Octreotide-soln treated group[1]. The serum level of gastrin is significantly reduced to around one-third of the baseline within two hours after taking an octreotide acetate test dose. This effect lasts for roughly six hours. Day 21: Octreotide acetatea (5 mg intramuscular, q 4 wk) is administered as part of a sustained-release formulation[2].
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| ln Vivo |
Tumor volume was significantly reduced in the octreotide-treated group compared with the saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) showed stronger antitumor effects than octreotide-solution (100 μg/kg, i.p.). Compared with the saline group, octreotide treatment had a significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC rats. Octreotide-PPSG seems to inhibit the expression of SSTR2 and SSTR5 more than the octreotide solution treatment group [1]. Test doses of octreotide acetate significantly reduced serum gastrin levels to approximately one-third of baseline within 2 hours, with effects lasting approximately 6 hours. On day 21, treatment with octreotide acetate extended-release formulation (5 mg intramuscularly, once every 4 weeks) was initiated [2].
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| Animal Protocol |
Mice: Three groups are randomly assigned to thirty mice bearing HCC xenografts: (A) Octreotide-soln group; (B) Octreotide-PPSG group; and (C) control group. The octreotide-soln group is given an intraperitoneal injection (i.p.) of 100 μg/kg octreotide-soln once a day for 14 days in a row. The Octreotide-PPSG group is administered a single subcutaneous injection with a volume of approximately 0.2 mL, containing 1.4 mg/kg of Octreotide-PPSG. Saline is injected intraperitoneally (i.p.) once daily for a total of 14 days to the control group. Following injection of H22 hepatoma cell suspension, treatment begins the following day and lasts for 14 days. Periodic caliper measurements are used to track the growth of tumors on days 7 and 14 after seeding. Equation can be used to calculate tumor volumes (V) from the tumor's length and width.
Rats: Two groups of twelve male SD rats are placed in standard cages at 25°C with free access to food and water one week before the experiment. Octreotide-PPSG or Octreotide-soln, at a single dose equivalent to 20 mg/kg, are injected subcutaneously into rats. The clinical dose of octreotide-soln in humans is used to calculate the dosage. The food is given back to the rats about two hours after the dosage, and they fast for twelve hours before. Heparinized Eppendorf tubes are used to collect blood samples at prearranged intervals. The blood samples are immediately placed on ice and centrifuged at 3000 g for 10 min in less than an hour after collection. Prior to analysis, the plasma is gathered and kept at -20°C. |
| References |
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| Molecular Formula |
C51H70N10O12S2
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|---|---|
| Molecular Weight |
1079.29
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| CAS # |
79517-01-4
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| Related CAS # |
Octreotide; 83150-76-9
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| Appearance |
Powder
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| 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
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| InChi Key |
DEQANNDTNATYII-OULOTJBUSA-N
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| InChi Code |
InChI=1S/C49H66N10O10S2/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/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)/t28-,29-,34-,36+,37+,38-,39-,40+,41+,42+/m1/s1
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| 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
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| Synonyms |
SMS 201-995 acetate; Octreotide acetate
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: ~250 mg/mL (~231.6 mM)
H2O: ~25 mg/mL (~23.2 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (2.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (2.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.25 mg/mL (2.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (92.65 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9265 mL | 4.6327 mL | 9.2654 mL | |
| 5 mM | 0.1853 mL | 0.9265 mL | 1.8531 mL | |
| 10 mM | 0.0927 mL | 0.4633 mL | 0.9265 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04941911 | Active Recruiting |
Drug: Octreotide Acetate Other: Placebo |
Liver Transplantation Renal Failure |
University College, London | May 27, 2022 | Phase 2 |
| NCT01613495 | Active Recruiting |
Drug: Placebo Drug: Octreotide |
Prader Willis Syndrome | Oregon Health and Science University | August 2005 | Not Applicable |
| NCT05364944 | Active Recruiting |
Drug: Debio 4126 Drug: Sandostatin LAR |
Acromegaly GEP-NET |
Debiopharm International SA | May 18, 2022 | Phase 1 |
| NCT00569127 | Active Recruiting |
Biological: Bevacizumab Drug: Octreotide Acetate |
Atypical Carcinoid Tumor Carcinoid Tumor |
National Cancer Institute (NCI) | December 1, 2007 | Phase 3 |
| NCT04125836 | Active Recruiting |
Drug: CAM2029 (octreotide subcutaneous depot) |
Acromegaly | Camurus AB | October 10, 2019 | Phase 3 |
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