| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
(Phenylac¹, D‑Tyr(Et)2, Lys⁶, Arg⁸, des‑Gly⁹)‑Vasopressin acetate targets the vasopressin V1a receptor (V1aR), a GPCR expressed on vascular smooth muscle cells, hepatocytes, and platelets. Activation of V1aR by vasopressin (arginine vasopressin, AVP) leads to vasoconstriction, glycogenolysis, and platelet aggregation. This peptide analogue contains multiple modifications: a phenylacetyl group at position 1 (instead of the native Tyr), D‑Tyr(Et) at position 2, Lys at position 6, Arg at position 8, and deletion of Gly⁹. These modifications confer V1a‑selective antagonism.
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| ln Vitro |
(Phenylac¹, D‑Tyr(Et)2, Lys⁶, Arg⁸, des‑Gly⁹)‑Vasopressin acetate is a synthetic vasopressin analogue and a selective antagonist of the vasopressin V1a receptor. No specific IC₅0 values for V1a receptor binding or functional antagonism are reported in the search results. The peptide was developed by Smith, Kline & French (SK&F) as a research tool to study V1a receptor physiology. It is also known by the code SK&F 101926. The acetate salt form improves solubility and handling.
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| ln Vivo |
No specific in vivo activity data for (Phenylac¹, D‑Tyr(Et)2, Lys⁶, Arg⁸, des‑Gly⁹)‑Vasopressin acetate are reported in the search results. As a selective V1a receptor antagonist, it has been used in animal studies to investigate the role of V1a receptors in blood pressure regulation, cardiac function, and renal water handling. The compound would be expected to block vasopressin‑induced vasoconstriction and reduce blood pressure in models of hypertension. However, no specific in vivo data are provided.
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| Enzyme Assay |
The binding of (Phenylac¹, D‑Tyr(Et)2, Lys⁶, Arg⁸, des‑Gly⁹)‑Vasopressin acetate to V1a receptors is measured by competitive radioligand binding assays using cell membranes expressing the V1a receptor. A radiolabeled vasopressin analog (e.g., [3H]‑AVP or [¹2⁵I]‑[Phe2, Ile⁴]‑AVP) is used as a tracer. The peptide is added at graded concentrations (0.1‑10,000 nM) to compete for binding, and the IC₅0 or Ki is calculated from dose‑response curves. For functional assays, V1a receptor activation is measured by intracellular calcium flux (using a fluorescent indicator) or by measuring inositol phosphate (IP) accumulation.
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| Cell Assay |
For cellular assays, cells expressing the V1a receptor (e.g., A7r5 rat aortic smooth muscle cells, or CHO‑V1aR cells) are seeded in 96‑well plates. For calcium assays, cells are loaded with Fluo‑4 AM. The peptide is added at graded concentrations (0.1‑10,000 nM) for 10‑30 min, then stimulated with vasopressin (1‑100 nM). The inhibition of the calcium signal is measured. For IP accumulation assays, cells are pre‑loaded with [3H]‑myo‑inositol, treated with the peptide, then stimulated with vasopressin. IP accumulation is measured by liquid scintillation counting. The IC₅0 is calculated.
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| Animal Protocol |
No animal experiments for this peptide are described in the search results. For in vivo evaluation of V1a antagonism, male Sprague‑Dawley rats would be used. The peptide would be administered intravenously (IV) at doses of 0.1‑10 mg/kg. Blood pressure and heart rate would be monitored via a carotid artery catheter. The vasopressor response to vasopressin (administered IV) would be measured before and after treatment with the antagonist. The compound would be expected to inhibit vasopressin‑induced pressor responses. No specific protocols are described.
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| ADME/Pharmacokinetics |
(Phenylac¹, D‑Tyr(Et)2, Lys⁶, Arg⁸, des‑Gly⁹)‑Vasopressin acetate (C₆₅H₉4N1₈O14·xC2H4O2, MW ≈ 1320 Da) is a lyophilized powder. For storage, the powder should be kept at -20 degC or -80 degC, sealed and protected from light. For in vitro use, stock solutions in water or PBS (1‑10 mg/mL) can be prepared and stored at -80 degC for up to 6 months or at -20 degC for 1 month. The acetate salt form improves solubility and handling. No detailed PK parameters are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for this peptide are reported. As a research‑grade peptide, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling peptides should be followed. V1a receptor antagonism can cause hypotension, which may be undesirable at high doses. No LD₅0 or formal toxicology studies are available.
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| References | |
| Additional Infomation |
This vasopressin analogue is a selective antagonist of the V1a receptor. Vasopressin (antidiuretic hormone, ADH) has multiple physiological actions mediated by three receptor subtypes: V1a (vascular smooth muscle, liver, platelets), V1b (pituitary, pancreas), and V2 (renal collecting duct). V1a receptor antagonists have been investigated as potential therapeutic agents for hypertension, heart failure, and Raynaud‘s phenomenon. This peptide antagonist, developed by Smith, Kline & French (SK&F 101926), is a research tool for V1a receptor studies. The compound is for research use only and has not received regulatory approval.
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| Molecular Formula |
C54H76N14O11.XC2H4O2
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| Molecular Weight |
1097.27 (free base)
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| Appearance |
Solid powder
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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 : 36.6 mg/mL
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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.) |
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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