| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Argipressin targets the vascular arginine vasopressin receptors (V1 receptors) located on vascular smooth muscle cells, as well as V2 receptors in the kidney. It binds to the V1 receptor with Kd values of 1.31 nM in A7r5 rat aortic smooth muscle cells and 1.44 nM in neonatal rat cardiomyocytes. Activation of V1 receptors causes vasoconstriction, while V2 receptor activation promotes water reabsorption in the kidneys.
|
|---|---|
| ln Vitro |
Arbopressin binds to A7r5 arterial aortic smooth muscle cells via vasopressin uptake V1, with a Kd of 1.31 nM. Additionally, it promotes immunological response against S-100 in non-cultured DRG cells, AVP-induced [Ca2+]i signaling, and intracellular calcium release in A7r5 cells (EC50=5 nM) [1]. The lowest effective dose of argipressin required to elicit a [Ca2+]i response in DRG cultured neuronal cells is 100 pM[2].
In vitro, argipressin binds to vascular arginine vasopressin receptor V1 with high affinity, with Kd values of 1.31 nM in A7r5 rat aortic smooth muscle cells and 1.44 nM in neonatal rat cardiomyocytes. The compound stimulates Ca²⁺ spiking activity in vascular smooth muscle cells via activation of phospholipase A2. It shows potent vasoconstrictive effects in isolated blood vessel preparations and promotes water transport in kidney cell models. |
| ln Vivo |
In vivo, argipressin is the primary antidiuretic hormone in mammals, regulating water balance by promoting water reabsorption in the kidney collecting ducts through V2 receptor activation. It also acts as a potent vasoconstrictor through V1 receptor activation, increasing peripheral vascular resistance and blood pressure. The hormone plays a crucial role in maintaining fluid homeostasis and cardiovascular function.
|
| Enzyme Assay |
For non-cell enzyme/receptor binding assays, argipressin binding to V1 and V2 receptors is assessed using membrane preparations from tissues expressing these receptors or from heterologous expression systems. Radioligand binding assays using [³H]arginine vasopressin or [¹²⁵I]labeled analogues are employed. Membrane fractions are incubated with the labeled ligand and varying concentrations of unlabeled argipressin. Bound and free ligand are separated by filtration, and Kd values are calculated from saturation and competition binding experiments.
|
| Cell Assay |
For in vitro cell-based assays, argipressin activity is assessed in cell lines expressing V1 or V2 receptors, such as A7r5 rat aortic smooth muscle cells or renal collecting duct cells. Cells are treated with argipressin at various concentrations, and receptor activation is measured by intracellular Ca²⁺ mobilization (for V1) or cAMP accumulation (for V2). Functional responses such as vasoconstriction in isolated vessels or water permeability in kidney cell models are also assessed.
|
| Animal Protocol |
For in vivo animal experiments, argipressin is typically administered intravenously or subcutaneously to animal models to assess its effects on blood pressure, urine output, and water balance. The compound is used in studies of diabetes insipidus, where its antidiuretic effects are evaluated. Cardiovascular effects are assessed by monitoring blood pressure and heart rate following administration. Dose-response studies are conducted to determine the potency and duration of action.
|
| ADME/Pharmacokinetics |
Argipressin has a molecular weight of 1084.23 g/mol and molecular formula C₄₆H₆₅N₁₅O₁₂S₂. It is a nonapeptide with two disulfide-linked cysteines. The compound is soluble in water at 100 mg/mL (92.23 mM). It should be stored at -20°C for long-term stability and transported with ice packs. The peptide is stable for at least 2 years under recommended storage conditions.
|
| Toxicity/Toxicokinetics |
Argipressin is generally well-tolerated at therapeutic doses. Adverse effects may include hypertension, bradycardia, and fluid retention due to its vasoconstrictive and antidiuretic properties. Overdose can lead to water intoxication, hyponatremia, and severe hypertension. The compound should be used with caution in patients with cardiovascular disease. It is approved for clinical use in the treatment of diabetes insipidus and certain bleeding disorders.
|
| References |
|
| Additional Infomation |
Arginine vasopressin is the major form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide with arginine at residue 8 and two disulfide-linked cysteine residues at residues 1 and 6. It has cardiovascular, hematologic, and mitogenic effects. It is the conjugate base of arginine vasopressin (2+). Arginine vasopressin is a synthetic peptide, similar to the endogenous nonapeptide hormone, and possesses antidiuretic properties. Synthesized in the hypothalamus and stored in/released from the posterior pituitary gland, arginine vasopressin's primary function is to regulate extracellular fluid volume. This substance can also act as a vasoconstrictor, increasing blood pressure and systemic vascular resistance. Arginine vasopressin is used to treat diabetes insipidus or to improve vasomotor tone and blood pressure.
Argipressin (arginine vasopressin) is the endogenous antidiuretic hormone in humans and is approved for clinical use. It is used to treat diabetes insipidus, to improve vasomotor tone, and as a vasopressor in septic shock. The compound is available as a pharmaceutical product for intravenous administration. Its mechanism involves V1 and V2 receptor activation. No new clinical trials are ongoing as it is an established therapeutic agent. |
| Molecular Formula |
C46H65N15O12S2
|
|---|---|
| Molecular Weight |
1084.23
|
| Exact Mass |
1083.437
|
| CAS # |
113-79-1
|
| Related CAS # |
Argipressin diacetate;75499-44-4;Argipressin acetate;129979-57-3
|
| PubChem CID |
644077
|
| Appearance |
White to off-white solid powder
|
| Density |
1.6±0.1 g/cm3
|
| Flash Point |
113℃
|
| Index of Refraction |
1.724
|
| LogP |
-5.99
|
| Hydrogen Bond Donor Count |
14
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
19
|
| Heavy Atom Count |
75
|
| Complexity |
2070
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
C1=CC=C(CC2NC(=O)C(CC3=CC=C(O)C=C3)NC(=O)C(N)CSSCC(C(N3C(C(NC(C(NCC(N)=O)=O)CCC/N=C(\N)/N)=O)CCC3)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC2=O)C=C1
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~92.23 mM)
|
|---|---|
| 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 | 0.9223 mL | 4.6116 mL | 9.2231 mL | |
| 5 mM | 0.1845 mL | 0.9223 mL | 1.8446 mL | |
| 10 mM | 0.0922 mL | 0.4612 mL | 0.9223 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.
Effets hémodynamiques de l’administration de vasopressine au décours de l’Arrêt Cardio-Respiratoire chez des patients en état de choc réfractaire
CTID: null
Phase: Phase 3 Status: Ongoing
Date: 2007-04-24
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
