| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Angiotensin receptor
Angiotensin acetate targets the angiotensin II receptor (AT1 receptor). It acts as an agonist at this receptor, mimicking the effects of endogenous angiotensin II. By binding to the AT1 receptor, it induces vasoconstriction, increases blood pressure, and stimulates aldosterone release. |
|---|---|
| ln Vitro |
In vitro, angiotensin acetate acts as an agonist at the angiotensin II receptor. It induces vasoconstriction in isolated blood vessels and stimulates signaling pathways in cells expressing the AT1 receptor. Its activity is assessed using receptor binding assays and functional assays measuring calcium mobilization or other downstream effects.
|
| ln Vivo |
Angiotensin II 5-valine infusion resulted in a significant increase in systolic blood pressure (SBP) by day 12 (197 ± 7 mm Hg). Losartan may prevent the development of hypertension associated with ANG II infusion. Blood and kidney samples were collected, HPLC was performed to separate angiotensin II 5-valine (exogenous) from Ile5-ANG II (endogenous), and the fractions were measured by radioimmunoassay. In the angiotensin II 5-valine infusion construct that received losartan treatment, total ANG II levels increased to a greater extent than in the waveform that did not receive lossartan treatment (289 ± 20 v 119 ± 14 fmol/ mL). However, Losartan significantly reduced the enhancement of renal Val5-ANG II content by 88%, and this enhancement occurred only in the specific gravity of Val5-ANG II [1].
In vivo, angiotensin acetate is used to study the effects of angiotensin II on blood pressure and fluid balance. It induces vasoconstriction and increases blood pressure. It also stimulates the release of aldosterone. Its effects are mediated through the AT1 receptor. |
| Enzyme Assay |
The in vitro receptor binding assay for angiotensin acetate typically involves radioligand displacement studies using membrane preparations from cells expressing the AT1 receptor. The compound's affinity is determined by measuring its ability to displace a specific radiolabeled ligand. Its functional activity as an agonist is assessed using assays measuring calcium mobilization or other downstream signaling.
|
| Cell Assay |
In vitro cellular assays for angiotensin acetate assess its functional activity as an AT1 receptor agonist. Cells expressing the AT1 receptor are treated with angiotensin acetate, and downstream signaling, such as calcium mobilization or ERK phosphorylation, is measured. These assays demonstrate the compound's potency and efficacy as an AT1 receptor agonist.
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| Animal Protocol |
In vivo animal studies for angiotensin acetate have been conducted to study its effects on blood pressure and fluid balance. However, specific details of these studies are not extensively detailed in the available literature. It is a research compound and is not approved for clinical use.
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| ADME/Pharmacokinetics |
Angiotensin acetate is a peptide that is administered by injection. It is rapidly metabolized in the body. Its pharmacokinetic properties are similar to those of angiotensin II. Specific parameters such as half-life are not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Angiotensin acetate is a potent vasoconstrictor and can cause significant increases in blood pressure. Its toxicity is related to its pharmacological activity. It should be handled with caution. It is not intended for human use.
|
| References | |
| Additional Infomation |
Val(5)-angiotensin II is an angiotensin II.
Angiotensin acetate is a biologically active peptide and a derivative of angiotensin II. It acts as an agonist at the AT1 receptor. It is used in research to study the renin-angiotensin system and the effects of angiotensin II. It is not approved for clinical use. |
| Molecular Formula |
C51H73N13O14
|
|---|---|
| Molecular Weight |
1092.222
|
| Exact Mass |
1031.518
|
| Elemental Analysis |
C, 56.08; H, 6.74; N, 16.67; O, 20.51
|
| CAS # |
58-49-1
|
| PubChem CID |
9811952
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.77
|
| Hydrogen Bond Donor Count |
13
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
28
|
| Heavy Atom Count |
74
|
| Complexity |
1960
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
NC(NCCC[C@H](NC([C@@H](N)CC(O)=O)=O)C(N[C@@H](C(C)C)C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@@H](C(C)C)C(N[C@@H](CC1=CN=CN1)C(N1[C@H](C(N[C@@H](CC2=CC=CC=C2)C(O)=O)=O)CCC1)=O)=O)=O)=O)=O)=N.CC(O)=O
|
| InChi Key |
JVCJXRGXGITABA-IAQGTVMASA-N
|
| InChi Code |
InChI=1S/C49H69N13O12.C2H4O2/c1-26(2)39(60-42(67)33(12-8-18-54-49(51)52)56-41(66)32(50)23-38(64)65)45(70)57-34(20-29-14-16-31(63)17-15-29)43(68)61-40(27(3)4)46(71)58-35(22-30-24-53-25-55-30)47(72)62-19-9-13-37(62)44(69)59-36(48(73)74)21-28-10-6-5-7-11-28;1-2(3)4/h5-7,10-11,14-17,24-27,32-37,39-40,63H,8-9,12-13,18-23,50H2,1-4H3,(H,53,55)(H,56,66)(H,57,70)(H,58,71)(H,59,69)(H,60,67)(H,61,68)(H,64,65)(H,73,74)(H4,51,52,54);1H3,(H,3,4)/t32-,33-,34-,35-,36-,37-,39-,40-;/m0./s1
|
| Chemical Name |
(2S,5S,8S,11S,14S,17S)-2-((1H-imidazol-4-yl)methyl)-17-amino-1-((S)-2-(((S)-1-carboxy-2-phenylethyl)carbamoyl)pyrrolidin-1-yl)-14-(3-guanidinopropyl)-8-(4-hydroxybenzyl)-5,11-diisopropyl-1,4,7,10,13,16-hexaoxo-3,6,9,12,15-pentaazanonadecan-19-oic acid compound with acetic acid (1:1)
|
| Synonyms |
Human Angiotensin II Acetate Salt; Val5-ANG II; H-Asp-Arg-Val-Tyr-Val-His-Pro-Phe-OH; Angiotensin acetate; (Val5)-Angiotensin II
|
| 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 (~96.9 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 33.33 mg/mL (32.29 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 | 0.9156 mL | 4.5778 mL | 9.1557 mL | |
| 5 mM | 0.1831 mL | 0.9156 mL | 1.8311 mL | |
| 10 mM | 0.0916 mL | 0.4578 mL | 0.9156 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00910923 | Completed | Drug: JNJ-38431055 | Diabetes Mellitus, Type 2 | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
November 2008 | Phase 1 |
| NCT01054118 | Completed | Drug: JNJ-38431055 Drug: Sitagliptin 100 mg |
Diabetes Mellitus, Type 2 | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
December 2009 | Phase 1 |
| NCT00871507 | Completed | Drug: JNJ-38431055 Dose 2 Drug: JNJ-38431055 Dose 1 |
Diabetes Mellitus, Type 2 | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
April 2009 | Phase 1 |