| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Angiotensin II receptors (AT1, AT2); G-protein coupled receptor (GPCR); Cardiovascular system; Blood pressure regulation
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|---|---|
| ln Vitro |
Saralasin (1 nM) inhibits 3T3 and SV3T3 cell proliferation for 48 or 72 hours [1]. Saralasin (5 μM, 2h) controls myocytes by fast restoring Ito, a transient outward K+ current in mouse ventricles that is rapidly inactivated, and slowly restoring IK, a transient outward K+ current in mouse ventricles that is slowly inactivated. levelReference [2]. With 74% of the binding sites having a Ki value of 0.32 nM and 74% having a Ki value of 2.7 nM, saralasin (0.1–10 nM, 40 min) blocked the binding of FITC-Ang II to a rat liver membrane preparation (used as a source of angiotensin receptors). remaining binding locations [3]. In vitro, saralasin (1 μM) perfused into rat ovaries decreases prostaglandin E2 and 6-ketoprostaglandin F1α levels and lowers the pace of ovulation [4].
Saralasin [(Sar1,Val5,Ala8)-Angiotensin II] is a partial agonist/competitive non-selective antagonist of angiotensin II receptors. It inhibits angiotensin II-mediated pressor effects. It is used in receptor binding assays and functional studies. |
| ln Vivo |
In cerulein-induced pancreatitis, saralasin (intravenous injection, 5–50 μg/kg, single dosage) reduces oxidative stress and tissue damage [5]. Saralasin, administered subcutaneously at a single dose of 10 and 30 mg/kg, elevates serum renin activity (SRA) in awake, normal rats without appreciably altering heart rate or blood pressure [6].
In vivo, Saralasin inhibits the pressor effects of angiotensin II in rats and shows blood pressure lowering activity in humans. It is used in animal models to study the RAS and hypertension. |
| Enzyme Assay |
For receptor binding assays, membranes from cells expressing angiotensin receptors are incubated with [125I]-angiotensin II and increasing concentrations of Saralasin. Bound ligand is separated by filtration and quantified.
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| 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. For cell-based assays, cells expressing angiotensin receptors are treated with Saralasin at various concentrations, and downstream signaling (calcium, inositol phosphate) is assessed. |
| 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. For in vivo studies, Saralasin is administered to rats or humans via intravenous infusion at doses ranging from 0.1-10 μg/kg/min. Blood pressure and pressor responses to angiotensin II are monitored. These protocols are for research purposes only. |
| References |
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| Molecular Formula |
C42H65N13O10
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|---|---|
| Molecular Weight |
912.046600000001
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| Exact Mass |
911.497
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| CAS # |
34273-10-4
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| Related CAS # |
Saralasin TFA;Saralasin acetate hydrate;39698-78-7
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| Sequence |
{Sar}-Arg-Val-Tyr-Val-His-Pro-Ala{Sar}-RVYVHPA
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| SequenceShortening |
{Sar}-RVYVHPA
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| Appearance |
White to off-white solid
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.654
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| LogP |
-0.27
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| SMILES |
CC([C@H](NC([C@@H](NC(CNC)=O)CCCNC(N)=N)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(O)=O)C)=O)=O)CC2=CN=CN2)=O)C(C)C)=O)CC3=CC=C(O)C=C3)=O)C
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| InChi Key |
PFGWGEPQIUAZME-NXSMLHPHSA-N
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| InChi Code |
InChI=1S/C42H65N13O10/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/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)/t24-,28-,29-,30-,31-,33-,34-/m0/s1
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| Chemical Name |
(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
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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) |
DMSO: ~50 mg/mL (~54.8 mM; with ultrasonication)
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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 | 1.0964 mL | 5.4822 mL | 10.9643 mL | |
| 5 mM | 0.2193 mL | 1.0964 mL | 2.1929 mL | |
| 10 mM | 0.1096 mL | 0.5482 mL | 1.0964 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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