Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Vapreotide (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 impact of SP on calcium release in a concentration-dependent manner. Vapreotide needs a concentration that is roughly 100 times greater than that of the NK1R antagonist aprepitant in order to fully block the effects of SP. SSTR2 is the main mediator of Vapreotide's effect on cell proliferation. U373MG cells are pretreated with SSTR2 selective antagonist CYN, then incubated with Vapreotide and stimulated with SP to further demonstrate the NK1R antagonist effect of Vapreotide. The findings demonstrate that the inhibitory effect of vapreotide on SP-stimulated IL-8 mRNA expression is not reversed by pretreatment with CYN. Vapreotide decreases HIV-1 replication in MDM, as seen by the reduced expression of HIV gag mRNA in comparison to control MDM. Furthermore, SP treatment (10 μM) reverses the inhibitory effect of vapreotide on HIV-1 replication in MDM. According to this observation, vapreotide's inhibition of HIV-1 replication is most likely caused by its interaction with NK1R[1].
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Cell Assay |
For 10 minutes, either Vapreotide (0, 5, 10, 20 μM) or SP are added, and then the HEK293-NK1R and U373MG cells are incubated for three hours. In some experiments, cells are stimulated with SP for three hours after being incubated with CYN for ten minutes, after which they are added to vapreotide and left to incubate for an extra ten. There are controls in the form of mock-treated cells[1].
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References |
Molecular Formula |
C57H70N12O9S2
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Molecular Weight |
1131.3707
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Exact Mass |
1130.48
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Elemental Analysis |
C, 60.51; H, 6.24; N, 14.86; O, 12.73; S, 5.67
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CAS # |
103222-11-3
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Related CAS # |
Vapreotide acetate; 849479-74-9; 936560-75-7 (diacetate)
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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
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InChi Key |
SWXOGPJRIDTIRL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C57H70N12O9S2/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/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)
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Chemical Name |
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 |
RC160; BMY 41606; BMY-41606; BMY41606; Vapreotide; Sanvar IR; Vapreotidum; RC 160; RC-160; RC160
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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 (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) |
H2O: ~100 mg/mL (~88.4 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 | 0.8839 mL | 4.4194 mL | 8.8388 mL | |
5 mM | 0.1768 mL | 0.8839 mL | 1.7678 mL | |
10 mM | 0.0884 mL | 0.4419 mL | 0.8839 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. th> |
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Vapreotide inhibits SP-induced IL-8 and MCP-1 expression in U373MG cells.Neuroimmunomodulation.2013;20(5):247-55. td> |