| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
Ornipressin acetate targets the vasopressin V1A receptor as an agonist. By binding to and activating V1 receptors, it induces vasoconstriction, which increases arterial blood pressure. The compound's vasoconstrictor and hemostatic effects are mediated through V1 receptor activation. It also has antidiuretic activity, which is mediated through V2 receptor activation. Ornipressin is a vasopressin agonist with specificity for the V1 receptor.
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|---|---|
| ln Vitro |
In vitro, ornipressin acetate acts as a vasopressin agonist specific for the V1 receptor. Its activity has been characterized in receptor binding and functional assays using cells expressing V1 receptors. The compound's ability to activate V1 receptor-mediated signaling, such as calcium mobilization, has been confirmed. It is a potent vasoconstrictor in isolated vascular preparations.
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| ln Vivo |
In vivo, ornipressin acetate increases arterial blood pressure in rats when administered at a dose of 0.1 nmol/kg. It is useful for skin hemostasis at a concentration of 10⁻² u/ml. This low concentration can reduce the total dose and side effects. Ornipressin acetate can be used as a local vasoconstrictor. It has antidiuretic activity.
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| Enzyme Assay |
In non-cell-based receptor binding assays, ornipressin acetate's affinity for vasopressin V1 receptors is evaluated using radioligand competition binding experiments. Membrane preparations from cells expressing recombinant human V1 receptors are incubated with a radiolabeled V1 receptor ligand and varying concentrations of ornipressin acetate. After incubation, bound and free radioligand are separated by filtration, and radioactivity is measured. Competition curves are generated to determine IC50 and Ki values. These assays confirm the compound's V1 receptor agonist activity.
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| Cell Assay |
In vitro cellular assays for ornipressin acetate involve measuring its agonist activity at V1 receptors in cultured cells. Cells expressing recombinant V1 receptors are treated with ornipressin acetate, and receptor activation is assessed by measuring downstream signaling such as calcium mobilization or inositol phosphate accumulation. The compound's ability to induce vasoconstriction is assessed using isolated vascular smooth muscle preparations. Its antidiuretic activity is assessed using kidney cell lines expressing V2 receptors.
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| Animal Protocol |
In vivo animal studies for ornipressin acetate have been conducted in rat models. The compound is typically administered via intravenous or local routes. Ornipressin acetate increases arterial blood pressure in rats when administered at a dose of 0.1 nmol/kg. It is useful for skin hemostasis at a concentration of 10⁻² u/ml. These studies confirm the compound's vasoconstrictor and hemostatic activity in vivo.
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| ADME/Pharmacokinetics |
Ornipressin acetate has a molecular formula of C45H63N13O12S2 · xC2H4O2. The compound is a synthetic peptide derivative of argipressin. It is a potent vasoconstrictor, hemostatic, and renal agent. The compound is typically stored as a powder at -20°C for long-term stability. Detailed pharmacokinetic parameters are available from preclinical studies.
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| Toxicity/Toxicokinetics |
As a research compound and potential therapeutic agent, ornipressin acetate should be handled with appropriate safety precautions. Comprehensive toxicology studies have been conducted as part of its development. The compound's vasoconstrictor effects may cause hypertension and other cardiovascular effects at high doses. It should be used with caution in patients with cardiovascular disease.
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| References |
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| Additional Infomation |
Ornipressin Acetate (POR-8 acetate) is a potent vasoconstrictor, hemostatic, and renal agent. It is a vasopressin agonist specific for the V1 receptor. Ornipressin acetate increases arterial blood pressure in rats and is useful for skin hemostasis. It has antidiuretic activity. The compound is a research agent and is not an approved drug in all regions.
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| Molecular Formula |
C47H67N13O14S2
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|---|---|
| Molecular Weight |
1102.25
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| Exact Mass |
1101.437
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| CAS # |
914453-98-8
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| Related CAS # |
914453-98-8 (acetate);3397-23-7;
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| PubChem CID |
66577106
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| Sequence |
Cys-Tyr-Phe-Gln-Asn-Cys-Pro-{Orn}-Gly-NH2 (Disulfide bridge: Cys1-Cys6)CYFQNCP-{Orn}-G-NH2 (Disulfide bridge: Cys1-Cys6)
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| SequenceShortening |
CYFQNCP-{Orn}-G-NH2 (Disulfide bridge: Cys1-Cys6)
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| Appearance |
White to off-white solid
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
76
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| Complexity |
1970
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| Defined Atom Stereocenter Count |
8
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| SMILES |
S1C[C@@H](C(N2CCC[C@H]2C(N[C@H](C(NCC(N)=O)=O)CCCN)=O)=O)NC([C@H](CC(N)=O)NC([C@H](CCC(N)=O)NC([C@H](CC2C=CC=CC=2)NC([C@H](CC2C=CC(=CC=2)O)NC([C@H](CS1)N)=O)=O)=O)=O)=O.OC(C)=O
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| InChi Key |
AYJSELDHDXYDKX-HPILINOVSA-N
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| InChi Code |
InChI=1S/C45H63N13O12S2.C2H4O2/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;1-2(3)4/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);1H3,(H,3,4)/t27-,28-,29-,30-,31-,32-,33-,34-;/m0./s1
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| Chemical Name |
H-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Orn-Gly-NH2 (Disulfide bond)
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| Synonyms |
Ornipressin Acetate Vasopressin8-L-ornithine-POR 8. 8-Ornithinevasopressin
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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) |
DMSO: ~16.7 mg/mL (with ultrasonication)
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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 | 0.9072 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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