| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
ACE 20 μM (IC50)
|
|---|---|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
In adult patients with sepsis or other distributive shock, serum angiotensin II levels were similar at baseline and 3 hours after intravenous infusion. Serum angiotensin I (the precursor peptide of angiotensin II) levels decreased by approximately 40% 3 hours after treatment. Official prescribing information indicates that there are currently no specific studies on angiotensin II clearance. Official prescribing information indicates that there are currently no specific studies on angiotensin II distribution. Official prescribing information indicates that angiotensin II clearance is independent of liver or kidney function. Metabolism/Metabolites In plasma, erythrocytes, and many major organs (such as the intestine, kidney, liver, and lung), angiotensin II is metabolized by aminopeptidase A and angiotensin-converting enzyme 2 to angiotensin-(2-8) [angiotensin III] and angiotensin-(1-7], respectively. Angiotensin III's activity mediated by the angiotensin II type 1 receptor (AT1) is approximately 40% that of angiotensin II; however, its aldosterone synthesis activity is similar to that of angiotensin II. Angiotensin-(1-7) acts on the AT1 receptor in the opposite way to angiotensin II, causing vasodilation. Nevertheless, official prescribing information also indicates that no formal studies have been conducted to investigate the metabolism of angiotensin II. Biological Half-Life The plasma half-life of intravenously injected angiotensin II is less than 1 minute. |
| References | |
| Additional Infomation |
Pharmacodynamics
Angiotensin II is a naturally occurring peptide hormone in the renin-angiotensin-aldosterone system (RAAS) that causes vasoconstriction and raises blood pressure. In the RAAS, juxtaglomerular cells in the afferent arterioles of the kidney synthesize the proteolytic enzyme renin. Although renin is stored in an inactive form called reninogen, a decrease in arterial blood pressure or extracellular fluid volume can trigger various enzymatic reactions that release active renin into the systemic circulation and peripheral tissues. This renin release results in the primary production of α2-globulin angiotensinogen in the liver, with smaller amounts produced in the kidneys and other organs. Angiotensin I itself is a relatively inactive decapeptide, produced from angiotensinogen and then rapidly converted to angiotensin II by angiotensin-converting enzyme (ACE). Therefore, angiotensin II exhibits potent vasopressor activity when rapidly degraded by aminopeptidases A and M into other substances such as angiotensin III and angiotensin IV. Angiotensin III and other substances can bind to and interact with specific G protein-coupled receptors (such as angiotensin receptor 1, AT-1), leading to strong vasoconstriction. Furthermore, in the ATHOS-3 clinical trial, 114 patients (70%) in the angiotensin II group reached their target mean arterial pressure (MAP) at 3 hours, with a median time to reach the target MAP endpoint of approximately 5 minutes. The dosage of angiotensin II was adjusted according to each patient's individual circumstances. |
| Molecular Formula |
C25H46N8O7
|
|---|---|
| Molecular Weight |
570.68
|
| Exact Mass |
570.348
|
| CAS # |
1226776-54-0
|
| PubChem CID |
172198
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.624
|
| LogP |
-0.57
|
| Hydrogen Bond Donor Count |
13
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
29
|
| Heavy Atom Count |
75
|
| Complexity |
1980
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
FC(C(=O)O)(F)F.O=C([C@H](C(C)C)NC([C@H](CCC/N=C(\N)/N)N)=O)N1CCC[C@H]1C(N[C@H](C(N[C@H](C(=O)O)CC(C)C)=O)CO)=O
|
| InChi Key |
CZGUSIXMZVURDU-JZXHSEFVSA-N
|
| InChi Code |
InChI=1S/C50H71N13O12/c1-5-28(4)41(47(72)59-36(23-31-25-54-26-56-31)48(73)63-20-10-14-38(63)45(70)60-37(49(74)75)22-29-11-7-6-8-12-29)62-44(69)35(21-30-15-17-32(64)18-16-30)58-46(71)40(27(2)3)61-43(68)34(13-9-19-55-50(52)53)57-42(67)33(51)24-39(65)66/h6-8,11-12,15-18,25-28,33-38,40-41,64H,5,9-10,13-14,19-24,51H2,1-4H3,(H,54,56)(H,57,67)(H,58,71)(H,59,72)(H,60,70)(H,61,68)(H,62,69)(H,65,66)(H,74,75)(H4,52,53,55)/t28-,33-,34-,35-,36-,37-,38-,40-,41-/m0/s1
|
| Chemical Name |
(3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[(2S)-2-[[(1S)-1-carboxy-2-phenylethyl]carbamoyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic 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)
|
| 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
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 | 1.7523 mL | 8.7615 mL | 17.5230 mL | |
| 5 mM | 0.3505 mL | 1.7523 mL | 3.5046 mL | |
| 10 mM | 0.1752 mL | 0.8761 mL | 1.7523 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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