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Purity: ≥98%
Vapreotide acetate (trade name: Sanvar) is a synthetic somatostatin analog and a NK1R antagonist with an IC50 of 330 nM. It is used to treat diarrhea associated with AIDS and esophageal variceal hemorrhage in patients with cirrhosis of the liver. The sequence of the eight-residue peptide is H-D-Phe-Cys(1)-Tyr-D-Trp-Lys-Val-Cys(1)-Trp-NH2.
| Targets |
NK1
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|---|---|
| ln Vitro |
Vapreotide reduces the intracellular calcium increases and NF-κB activation triggered by Substance P (SP) in a dose-dependent manner. Additionally, vapreotide prevents HEK293-NK1R and U373MG cell lines from producing MCP-1 and IL-8 in response to SP. When SP pretreatment is applied, the inhibitory effect of vapreotide on HIV-1 infection of human MDM in vitro can be reversed]. Human pituitary adenoma cells that secrete GH are strongly inhibited by vapreotide at concentrations as low as 10-12-10-14 M from releasing GH, PRL, and/or alpha-subunits. An IC50 of 0.1 pM is required for vapreotide to inhibit GH release[2]. Vapreotide has low affinity for SSTR1 and -4 (IC50=200 and 620 nM, respectively) and moderate-to-high affinities for SSTR2, -3, and -5 (IC50=0.17, 0.1, and 21 nM, respectively). The proliferation of CHO cells expressing SSTR2 and SSTR5 (EC50=53 and 150 pM, respectively) is inhibited by RC-160 when exposed to serum[3].
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| ln Vivo |
Oesophagogastric varices rupturing, which causes bleeding, is a serious side effect of portal hypertension in cirrhosis. When rats are given vapreotide acutely, their collateral circulation blood flow is reduced, and when they are given it chronically, its development is attenuated[4]. When administered subcutaneously at a dose of 100 μg/day/animal, RC-160 reduces tumor volumes and weights by approximately 40%. When medication is initiated early in the tumor's development, dipreotide can slow the growth of androgen-independent prostate cancer[5].
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| Cell Assay |
In aMEM supplemented with 10% FCS, CHO cells are cultivated. A MEM containing 10% FCS or insulin with or without vapreotide is used as the attachment medium after an overnight stay. With a Coulter counter model ZM, cells are counted to determine cell growth after 24 hours[3].
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| Animal Protocol |
Rats: Acute effects in DMNA rats are assessed at baseline and 30 minutes after vapreotide (8 μg/kg/hr) or placebo infusions. Subcutaneous implants are used to assess chronic hemodynamic effects in anesthetized DMNA rats and sham rats over a five-week period. The combined dilution–TTU method and the transit time ultrasound method are two methods used to measure hemodynamic parameters, including splenorenal shunt blood flow[4].
Mice: For four weeks, somatostatin analog vapreotide (20 μg/day/animal), bombesin/gastrin-releasing peptide (GRP) antagonist, or a combination of both peptides, are administered to nude mice containing xenografts of the androgen-independent human prostate-cancer cell line PC-3. Tumor weights and volumes are quantified [5]. |
| References |
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| Molecular Formula |
C59H74N12O11S2
|
|---|---|
| Molecular Weight |
1191.42267084122
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| Exact Mass |
1190.5
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| Elemental Analysis |
C, 59.48; H, 6.26; N, 14.11; O, 14.77; S, 5.38
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| CAS # |
849479-74-9
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| Related CAS # |
Vapreotide; 103222-11-3
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| Appearance |
Solid powder
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| SMILES |
CC(C)C1C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)C(CC5=CC=CC=C5)N)C(=O)NC(CC6=CNC7=CC=CC=C76)C(=O)N.CC(=O)O
|
| InChi Key |
KBIZSMHYSQUHDH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C57H70N12O9S2.C2H4O2/c1-32(2)49-57(78)68-48(55(76)64-44(50(60)71)26-35-28-61-41-16-8-6-14-38(35)41)31-80-79-30-47(67-51(72)40(59)24-33-12-4-3-5-13-33)56(77)65-45(25-34-19-21-37(70)22-20-34)53(74)66-46(27-36-29-62-42-17-9-7-15-39(36)42)54(75)63-43(52(73)69-49)18-10-11-23-58;1-2(3)4/h3-9,12-17,19-22,28-29,32,40,43-49,61-62,70H,10-11,18,23-27,30-31,58-59H2,1-2H3,(H2,60,71)(H,63,75)(H,64,76)(H,65,77)(H,66,74)(H,67,72)(H,68,78)(H,69,73);1H3,(H,3,4)
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| Chemical Name |
acetic acid;10-(4-aminobutyl)-N-[1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-19-[(2-amino-3-phenylpropanoyl)amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
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| Synonyms |
BMY-41606; BMY 41606; BMY41606; RC160; RC 160; RC-160; DP-05-094; Octastatin; Vapreotide acetate
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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) |
H2O: ~14.3 mg/mL (~12 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 | 0.8393 mL | 4.1967 mL | 8.3933 mL | |
| 5 mM | 0.1679 mL | 0.8393 mL | 1.6787 mL | |
| 10 mM | 0.0839 mL | 0.4197 mL | 0.8393 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.
Vapreotide attenuates SP-induced NF-κB activation and IL-8, EGR-1 and c-Fos mRNA up-regulation in HEK293-NK1R cells.Neuroimmunomodulation.2013;20(5):247-55. |
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Vapreotide inhibits SP-induced IL-8 and MCP-1 expression in U373MG cells.Neuroimmunomodulation.2013;20(5):247-55. |
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