![Lysipressin acetate (Lysine vasopressin acetate; [Lys8]-Vasopressin acetate)](/upload/1124/V74621.png)
| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Arginine vasopressin receptor 1A (V1A receptor). Lysipressin acetate is a potent agonist of the V1A receptor. It binds to rat and human V1A receptors with high affinity, exhibiting Ki values of 1.2 nM and 10.1 nM, respectively. By activating this receptor, the compound mediates vasoconstriction and other physiological effects. It also induces contraction of smooth muscle and activates adenylate cyclase.
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| ln Vitro |
Lysipressin acetate is a potent agonist of the V1A receptor, with Ki values of 1.2 nM and 10.1 nM for the rat and human receptors, respectively. It induces contraction of rabbit urinary bladder smooth muscle and activates adenylate cyclase. In cultured rat and human vascular smooth muscle cells (VSMCs), it increases intracellular calcium levels.
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| ln Vivo |
In vivo, Lysipressin acetate functions as an antidiuretic hormone, promoting water retention in the body and constricting blood vessels. As a V1A receptor agonist, it is used in research to study the physiological roles of vasopressin, such as blood pressure regulation, water homeostasis, and smooth muscle contraction. Its effects are mediated through the activation of the V1A receptor and subsequent signaling pathways.
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| Enzyme Assay |
In vitro binding assays are used to characterize the interaction of Lysipressin acetate with the V1A receptor. Typically, radioligand binding assays are performed using membranes from cells expressing the rat or human V1A receptor. The compound's ability to displace a labeled V1A antagonist is measured to determine its binding affinity (Ki). For Lysipressin acetate, Ki values of 1.2 nM (rat) and 10.1 nM (human) have been reported.
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| Cell Assay |
Cellular assays for Lysipressin acetate involve treating cells expressing the V1A receptor, such as vascular smooth muscle cells, with the compound. The activation of the receptor is then measured by assessing downstream signaling events, such as an increase in intracellular calcium levels. This confirms the compound's agonistic activity and allows for the characterization of its potency and efficacy in a cellular context.
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| Animal Protocol |
In vivo studies with Lysipressin acetate are typically performed in animal models to study vasopressin physiology. The compound can be administered to assess its effects on blood pressure, water balance, and smooth muscle contraction. Its antidiuretic and vasoconstrictive properties make it a useful tool for investigating the role of the V1A receptor in various physiological and pathophysiological processes.
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| ADME/Pharmacokinetics |
Lysipressin acetate is a peptide hormone analog with the molecular formula C48H69N13O14S2. Its pharmacokinetic properties, such as a short half-life due to rapid degradation by peptidases, are characteristic of peptide hormones. It is typically administered via injection for in vivo studies. Its activity is mediated through its binding and activation of the V1A receptor.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for Lysipressin acetate. As a vasopressin analog, its toxicity profile would be related to its pharmacological effects. Overdosing could lead to excessive vasoconstriction, hypertension, or water intoxication (hyponatremia). Its use is restricted to research applications, and it is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
Lysipressin acetate (Lysine vasopressin acetate, CAS#: 83968-49-4) is a peptide analog of vasopressin and a potent agonist of the V1A receptor. It has Ki values of 1.2 nM and 10.1 nM for rat and human V1A receptors, respectively. It induces smooth muscle contraction and activates adenylate cyclase. It is a research tool for studying vasopressin receptor function and is not approved for clinical use.
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| Molecular Formula |
C48H69N13O14S2
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| Molecular Weight |
1116.27
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| Exact Mass |
1115.452
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| CAS # |
83968-49-4
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| Related CAS # |
Lysipressin;50-57-7
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| PubChem CID |
91844584
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| Appearance |
White to off-white solid powder
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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 |
19
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| Heavy Atom Count |
77
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| Complexity |
1990
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC(=O)O.C1C[C@H](N(C1)C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N
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| InChi Key |
NKWAIKZITYLOMT-DHSVNZEYSA-N
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| InChi Code |
InChI=1S/C46H65N13O12S2.C2H4O2/c47-17-5-4-9-29(40(65)52-22-38(51)63)54-45(70)35-10-6-18-59(35)46(71)34-24-73-72-23-28(48)39(64)55-31(20-26-11-13-27(60)14-12-26)43(68)56-32(19-25-7-2-1-3-8-25)42(67)53-30(15-16-36(49)61)41(66)57-33(21-37(50)62)44(69)58-34;1-2(3)4/h1-3,7-8,11-14,28-35,60H,4-6,9-10,15-24,47-48H2,(H2,49,61)(H2,50,62)(H2,51,63)(H,52,65)(H,53,67)(H,54,70)(H,55,64)(H,56,68)(H,57,66)(H,58,69);1H3,(H,3,4)/t28-,29-,30-,31-,32-,33-,34-,35-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-N-[(2S)-6-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxohexan-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) |
DMSO: ≥ 100 mg/mL (89.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8958 mL | 4.4792 mL | 8.9584 mL | |
| 5 mM | 0.1792 mL | 0.8958 mL | 1.7917 mL | |
| 10 mM | 0.0896 mL | 0.4479 mL | 0.8958 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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