| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
| Targets |
Ornipressin is a vasopressin agonist that specifically targets the V1 receptor, a G protein-coupled receptor located on the smooth muscle cells of blood vessels. By binding to these V1 receptors, Ornipressin triggers vasoconstriction, which leads to increased blood pressure and reduced blood flow. It has an EC50 of 0.35 nM for the rat vasopressin V1a receptor and an EC50 of 7.5 nM for the human V1b receptor. It also shows agonist activity at the human oxytocin receptor with an EC50 of 71 nM. Its specificity for the V1 receptor over other vasopressin receptor subtypes makes it effective as a local vasoconstrictor.
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| ln Vitro |
In vitro, Ornipressin's activity is characterized by its potent agonism at vasopressin receptors. In cellular assays using CHO-K1 cells, it exhibits an EC50 of 71 nM for the human oxytocin receptor. In Flp-In-293 cells, it shows an EC50 of 7.5 nM for the recombinant human vasopressin V1b receptor. Its highest potency is observed at the rat vasopressin V1a receptor, with an EC50 of 0.35 nM in HEK293 cells. These functional assays, typically using luciferase reporter gene systems, demonstrate Ornipressin's ability to activate these receptors and initiate downstream signaling cascades that lead to its vasoconstrictive effects.
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| ln Vivo |
In vivo, Ornipressin acts as a potent systemic and local vasoconstrictor. It is used to reverse hypotension associated with combined general/epidural anesthesia. In patients with hepatorenal syndrome type 1, Ornipressin in combination with dopamine has been shown to be a useful therapeutic option, often serving as a bridge to liver transplantation. It can help reduce blood flow in the veins of the gastrointestinal tract, potentially controlling bleeding from varices. It is administered intravenously to achieve these effects, as its primary action is on the vascular smooth muscle to induce vasoconstriction.
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| Enzyme Assay |
Cell-free receptor binding assays for Ornipressin typically use membrane preparations from cells expressing recombinant vasopressin receptors. A common protocol involves incubating the receptor-containing membranes with a radiolabeled ligand, such as [3H]-arginine vasopressin, and varying concentrations of Ornipressin. Bound and free ligand are separated by filtration or centrifugation, and the radioactivity is measured by scintillation counting. The binding affinity (Ki) is determined by competitive displacement curves. Alternatively, surface plasmon resonance (SPR) can be used to study the direct interaction between Ornipressin and immobilized V1 receptors without the need for radiolabels.
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| Cell Assay |
For in vitro cellular experiments, cells such as CHO-K1, Flp-In-293, or HEK293 cells stably expressing vasopressin or oxytocin receptors are used. Cells are seeded in multi-well plates and treated with Ornipressin at various concentrations (typically 0.01-1000 nM). Receptor activation is assessed using a luciferase reporter gene assay, where receptor activation drives the expression of a luciferase gene. After incubation, a luciferase substrate is added, and the luminescence is measured. The EC50 value, representing the concentration of Ornipressin required for half-maximal receptor activation, is calculated from the dose-response curve.
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| Animal Protocol |
In vivo animal experiments with Ornipressin are typically conducted in rodent models to study its vasoconstrictive and hemostatic effects. A common protocol involves inducing hypotension in anesthetized rats or mice, followed by intravenous administration of Ornipressin at various doses (e.g., 0.1-10 ug/kg). Blood pressure and heart rate are continuously monitored using a pressure transducer. The compound's efficacy is assessed by its ability to restore blood pressure to baseline levels. For hemostasis studies, a bleeding model (e.g., tail transection or liver laceration) is used, and the time to hemostasis and blood loss are measured after Ornipressin administration.
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| ADME/Pharmacokinetics |
Ornipressin has a molecular weight of 1042.19 g/mol and a molecular formula of C45H63N13O12S2. As a peptide, it is administered intravenously and has a short half-life in circulation due to rapid proteolytic degradation. It is typically formulated as a sterile solution for injection. Its pharmacokinetic profile is characterized by rapid onset of action and a relatively short duration of effect, necessitating careful titration for clinical use. It is soluble in water and should be stored under appropriate conditions to maintain stability.
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| Toxicity/Toxicokinetics |
The toxicity profile of Ornipressin is related to its potent vasoconstrictive effects. Adverse effects can include hypertension, bradycardia, and peripheral ischemia due to excessive vasoconstriction. In the context of hepatorenal syndrome, its use is often limited by these cardiovascular side effects. It can also cause abdominal cramps and nausea due to its effects on smooth muscle. The compound is for research use only and not for human therapeutic use. Due to its potency, it should be handled with care in a controlled laboratory environment using appropriate safety precautions.
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| Additional Infomation |
Ornipressin is an oligopeptide. It is a synthetic analog of vasopressin, in which the 8th residue of the cyclic nonapeptide is replaced by ornithine. It is used as a local vasoconstrictor and hemostatic agent.
Ornipressin (POR-8) is a synthetic analog of vasopressin with the 8th residue replaced by ornithine. It is a potent vasoconstrictor, hemostatic, and renal agent. Its primary mechanism is via specific agonism of the V1 receptor, leading to vasoconstriction and increased blood pressure. It has been studied for its ability to reverse hypotension and as a treatment for hepatorenal syndrome. Despite its clinical potential, its use is often limited by its side effect profile. It is a controlled substance and is not approved for sale in some territories. It is intended for research use only. |
| Molecular Formula |
C45H63N13O12S2.C2H4O2
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| Molecular Weight |
1102.24358
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| Exact Mass |
1041.416
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| CAS # |
3397-23-7
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| PubChem CID |
14257660
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1616.2±65.0 °C at 760 mmHg
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| Flash Point |
931.3±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.583
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| LogP |
-5.66
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
72
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| Complexity |
1940
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| Defined Atom Stereocenter Count |
8
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| SMILES |
O=C([C@H]1N(C([C@@H](NC([C@H](CC(N)=O)NC([C@H](CCC(N)=O)NC([C@H](CC2=CC=CC=C2)NC([C@H](CC3=CC=C(O)C=C3)N4)=O)=O)=O)=O)CSSC[C@H](N)C4=O)=O)CCC1)N[C@@H](CCCN)C(NCC(N)=O)=O
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| InChi Key |
MUNMIGOEDGHVLE-LGYYRGKSSA-N
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| InChi Code |
InChI=1S/C45H63N13O12S2/c46-16-4-8-28(39(64)51-21-37(50)62)53-44(69)34-9-5-17-58(34)45(70)33-23-72-71-22-27(47)38(63)54-30(19-25-10-12-26(59)13-11-25)42(67)55-31(18-24-6-2-1-3-7-24)41(66)52-29(14-15-35(48)60)40(65)56-32(20-36(49)61)43(68)57-33/h1-3,6-7,10-13,27-34,59H,4-5,8-9,14-23,46-47H2,(H2,48,60)(H2,49,61)(H2,50,62)(H,51,64)(H,52,66)(H,53,69)(H,54,63)(H,55,67)(H,56,65)(H,57,68)/t27-,28-,29-,30-,31-,32-,33-,34-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
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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 : ~75 mg/mL (~71.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (47.98 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9072 mL | 4.5362 mL | 9.0724 mL | |
| 5 mM | 0.1814 mL | 0.9072 mL | 1.8145 mL | |
| 10 mM | 0.0907 mL | 0.4536 mL | 0.9072 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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