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Physicochemical Properties
| Molecular Formula | C40H54N8O8 |
| Molecular Weight | 774.90556 |
| Exact Mass | 774.406 |
| CAS # | 12676-15-2 |
| Related CAS # | Angiotensin II (3-8), human TFA |
| PubChem CID | 123814 |
| Appearance | Typically exists as solid at room temperature |
| LogP | 3.389 |
| Hydrogen Bond Donor Count | 8 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 19 |
| Heavy Atom Count | 56 |
| Complexity | 1340 |
| Defined Atom Stereocenter Count | 7 |
| SMILES | CC[C@@H]([C@@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@@H](CC1C=CC=CC=1)C(=O)O)=O)=O)CC1=CNC=N1)=O)NC([C@H](CC1C=CC(O)=CC=1)NC([C@H](C(C)C)N)=O)=O)C |
| InChi Key | QSBGWDDCOJYQGY-KOQODJNWSA-N |
| InChi Code | InChI=1S/C40H54N8O8/c1-5-24(4)34(47-35(50)29(44-37(52)33(41)23(2)3)18-26-13-15-28(49)16-14-26)38(53)45-30(20-27-21-42-22-43-27)39(54)48-17-9-12-32(48)36(51)46-31(40(55)56)19-25-10-7-6-8-11-25/h6-8,10-11,13-16,21-24,29-34,49H,5,9,12,17-20,41H2,1-4H3,(H,42,43)(H,44,52)(H,45,53)(H,46,51)(H,47,50)(H,55,56)/t24-,29-,30-,31-,32-,33-,34-/m0/s1 |
| Chemical Name | (2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid |
| 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 |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | Acts as a less effective agonist at the AT₁ receptor compared to Angiotensin II (AII) or Angiotensin III (AIII). The study found no evidence for interaction with a novel, losartan-insensitive receptor as previously suggested. [1] |
| ln Vivo |
Rats under anesthesia exhibit endothelium-dependent renal cortical vasodilation when exposed to human angiotensin II (3–8). At dosages of 1.25 and 12.5 nmol/kg, human angiotensin II (3–8) causes renal impairment and a dose-dependent rise in mean arterial blood pressure, but it has no cardiovascular effects at doses up to 125 pmol/kg. flow and vascular conductance are decreased by and mesenteric blood pressure [1]. In conscious Long Evans rats, intravenous bolus administration of Angiotensin II (3-8), human (0.125, 1.25, and 12.5 nmol/kg) caused dose-dependent increases in mean arterial blood pressure. [1] These pressor effects were accompanied by dose-dependent reductions in renal and mesenteric blood flow and vascular conductance. The dose-effect relationship was particularly steep in the renal vascular bed. [1] The cardiovascular effects (pressor and vasoconstrictor responses) of Angiotensin II (3-8), human (12.5 nmol/kg) were completely abolished by pretreatment with the AT₁ receptor antagonist losartan (20 μmol/kg, i.v. bolus). [1] Pretreatment with a primed infusion of L-arginine (1.4 mmol/kg bolus + 1.4 mmol/kg/h infusion) did not consistently alter the hemodynamic responses to Angiotensin II (3-8), human (12.5 nmol/kg). [1] The pressor and vasoconstrictor effects of Angiotensin II (3-8), human were similar in pattern to those of AII and AIII but were approximately 100-fold less potent and of considerably shorter duration. [1] |
| Animal Protocol |
Surgical Preparation: Male Long Evans rats (350-450 g) were anesthetized. Pulsed Doppler flow probes were implanted around the left renal artery, superior mesenteric artery, and distal abdominal aorta to measure regional blood flow. After a 7-14 day recovery, catheters were implanted in the distal abdominal aorta (for blood pressure measurement) and the right jugular vein (for drug administration). [1] Drug Administration and Hemodynamic Measurement: On experimental days, conscious, freely moving rats received intravenous bolus injections of Angiotensin II (3-8), human (dissolved in sterile isotonic saline containing 1% bovine serum albumin) at doses of 0.125, 1.25, and 12.5 nmol/kg (in a volume of 100 μL, flushed with 100 μL saline). Injections were separated by at least 20 minutes. Continuous recordings of heart rate, mean arterial blood pressure, and regional Doppler shift signals (converted to flow and vascular conductance) were made. Data were analyzed over specific time periods following administration. [1] Pharmacological Intervention Studies: In separate experiments, responses to Angiotensin II (3-8), human (12.5 nmol/kg) were assessed before and 5 minutes after an intravenous bolus of losartan (20 μmol/kg). In another set, responses were assessed before and 5 minutes after the start of a primed infusion of L-arginine (1.4 mmol/kg bolus followed by 1.4 mmol/kg/h infusion). [1] |
| References |
[1]. Regional haemodynamic effects of angiotensin II (3-8) in conscious rats. Br J Pharmacol. 1993 Sep;110(1):159-62. |
| Additional Infomation |
Angiotensin IV is an organic molecular entity. Angiotensin II (3-8), human (H2N-Val-Tyr-Ile-His-Pro-Phe-OH), also known as Angiotensin IV, is a degradation product of Angiotensin II. [1] This study in conscious rats found no evidence for the vasodilator effect of Angiotensin II (3-8), human in renal or mesenteric vascular beds as reported by others in anesthetized models. Instead, it elicited AT₁ receptor-mediated vasoconstriction. [1] The results suggest that Angiotensin II (3-8), human acts as a weak, short-acting agonist at the AT₁ receptor, providing no functional support for the existence of a unique, losartan-insensitive "Angiotensin IV" receptor under these experimental conditions. [1] |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2905 mL | 6.4524 mL | 12.9047 mL | |
| 5 mM | 0.2581 mL | 1.2905 mL | 2.5809 mL | |
| 10 mM | 0.1290 mL | 0.6452 mL | 1.2905 mL |