| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The target is the angiotensin II receptor (AT1 subtype). Saralasin competes with angiotensin II for receptor binding, blocking angiotensin II–mediated vasoconstriction and aldosterone secretion. Its partial agonist activity can produce transient agonistic effects, particularly when angiotensin II levels are low.
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|---|---|
| ln Vitro |
Cell proliferation of 3T3 and SV3T3 cells is inhibited by saralisin acetate hydrate (1 nM, 48 or 72 hours) [1]. Ito (a transient outward K+ current in rapidly inactivating mouse ventricles) and slow IK (a transient outward K+ current in slowly inactivating mouse ventricles) and Control levels in muscle cells are promptly restored by saralazine acetate hydrate (5 μM, 2 hours)[2]. The binding of FITC-Ang II to a rat liver membrane preparation (used as a source of angiotensin receptors) is inhibited by saralasin acetate hydrate (0.1–10 nM, 40 min), with a Ki value of 0.32 for 74% of the binding sites nM and a Ki value of 2.7 nM for the remaining binding sites [3]. When compared to a control group, prostaglandin E2 and 6-keto prostaglandin F1α levels are decreased and the ovulation rate is inhibited by 1 μM of salamelan acetate hydrate perfused in rat ovaries in vitro [4].
Saralasin binds AT1 receptors with high affinity and competitively inhibits angiotensin II–induced signaling. Its partial agonist activity is evident in systems with low angiotensin II tone, and its antagonist potency is expressed as a shift in the angiotensin II dose-response curve. |
| ln Vivo |
Saracin acetate hydrate (intravenous injection, 5-50 μg/kg, single dosage) reduces oxidative stress and tissue damage in cerulein-induced pancreatitis [5]. Saralasin acetate hydrate (subcutaneous injection, 10 and 30 mg/kg, single dose) increases serum renin activity (SRA) in normal, awake rats without significantly affecting blood pressure or heart rate [6].
In humans, saralasin lowers blood pressure and aldosterone levels in proportion to circulating renin and angiotensin II, enabling identification of renin-dependent hypertension. It was approved as a diagnostic probe and later withdrawn after orally active ACE inhibitors became available. |
| Enzyme Assay |
Receptor binding is measured using AT1-expressing cell membranes and a radiolabeled angiotensin II analogue (e.g., [125I]Sar1,Ile8-AngII); competition curves with saralasin yield Ki values. Functional antagonism is assessed by angiotensin II–induced calcium mobilization or inositol phosphate accumulation in AT1-expressing cells.
|
| Cell Assay |
Cell proliferation assay [1]
Cell Types: 3T3 and SV3T3 Cell Tested Concentrations: 1 nM Incubation Duration: 48 hrs (hours), 72 hrs (hours) Experimental Results: Inhibited cell growth of 3T3 and SV3T3 cells and caused an increase in cellular renin concentration. AT1-expressing cells (e.g., vascular smooth muscle cells or transfected HEK293 cells) are treated with saralasin in the presence of angiotensin II; intracellular calcium is measured by fluorescence imaging, and receptor internalization is assessed by flow cytometry or immunoblotting. |
| Animal Protocol |
Animal/Disease Models: Cerulein-induced acute pancreatitis rat model [5]
Doses: 5, 10, 20, 50 μg/kg, single dose. Mode of Route of Administration: intravenous (iv) (iv)injection. Experimental Results: The morphological characteristics of the pancreas returned to control levels. Reduces pancreatic damage and inhibits azure-induced glutathione depletion. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat [6] Doses: 10 and 30 mg/kg, single dose. Route of Administration: subcutaneous injection Experimental Results: Stimulates renin release without changing blood pressure or heart rate when serum renin levels are measured 20 minutes after injection. In humans, saralasin is administered by intravenous infusion with blood pressure monitoring, and plasma renin activity and aldosterone are measured to assess renin dependence. In animals, saralasin is infused intravenously in angiotensin II–dependent hypertension models, and blood pressure and aldosterone responses are recorded. |
| References |
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| Additional Infomation |
An angiotensin II (bovine) octapeptide analogue, with its amino acids at positions 1 and 8 replaced by sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II used for the diagnosis of hypertension.
See also: Salazine acetate (note moved to). |
| Molecular Formula |
C44H71N13O13
|
|---|---|
| Molecular Weight |
990.113849878311
|
| Exact Mass |
989.529
|
| CAS # |
39698-78-7
|
| Related CAS # |
Saralasin TFA;Saralasin;34273-10-4
|
| PubChem CID |
11954381
|
| Sequence |
{Sar}-RVYVHPA
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
14
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
25
|
| Heavy Atom Count |
70
|
| Complexity |
1700
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C[C@@H](C(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC2=CN=CN2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC3=CC=C(C=C3)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC.CC(=O)O.O
|
| InChi Key |
YBZYNINTWCLDQA-UHKVWXOHSA-N
|
| InChi Code |
InChI=1S/C42H65N13O10.C2H4O2.H2O/c1-22(2)33(53-35(58)28(50-32(57)20-45-6)9-7-15-47-42(43)44)38(61)51-29(17-25-11-13-27(56)14-12-25)36(59)54-34(23(3)4)39(62)52-30(18-26-19-46-21-48-26)40(63)55-16-8-10-31(55)37(60)49-24(5)41(64)65;1-2(3)4;/h11-14,19,21-24,28-31,33-34,45,56H,7-10,15-18,20H2,1-6H3,(H,46,48)(H,49,60)(H,50,57)(H,51,61)(H,52,62)(H,53,58)(H,54,59)(H,64,65)(H4,43,44,47);1H3,(H,3,4);1H2/t24-,28-,29-,30-,31-,33-,34-;;/m0../s1
|
| Chemical Name |
acetic acid;(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid;hydrate
|
| 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)
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| 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
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0100 mL | 5.0499 mL | 10.0999 mL | |
| 5 mM | 0.2020 mL | 1.0100 mL | 2.0200 mL | |
| 10 mM | 0.1010 mL | 0.5050 mL | 1.0100 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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