| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
In vitro, plasma renin activity (PRA) is inhibited by aliskiren hydrochloride at IC50 values of 2.9 nM for human PRA and 8.0 nM for monkey PRA [1]. Human aortic smooth muscle cells' prorenin-induced migration is inhibited by aliskiren hydrochloride (10 μM; 24 h) [2]. While prorenin-induced morphological alterations and lamellipodia production are inhibited by Aliskiren hydrochloride (1–10 μM; 24 hours), PDGF-BB activity is not significantly affected [2].
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| ln Vivo |
In marmosets lacking in sodium, aliskiren hydrochloride (3 mg/kg, 10 mg/kg; oral; daily; 0–12 days) inhibits renin and lowers blood pressure without changing heart rate [3]. In mice, aliskiren hydrochloride (10 mg/kg; oral; single dose) decreases tumors, postpones the onset of cachexia, and increases survival time. Moreover, it can boost physical activity, prevent muscle atrophy, and increase general body strength, mobility, and coordination [4]. Twenty days following C26 injection, a single oral dose of 10 mg/kg of aliskiren hydrochloride is administered to alleviate the oxidative stress linked to cancer cachexia [4].
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| Cell Assay |
Cell migration assay[2]
Cell Types: Smooth muscle cells (SMC) Tested Concentrations: 1-10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Prorenin (10 nM) at 10 μM inhibits human aortic smooth muscle cell migration. |
| Animal Protocol |
Animal/Disease Models: Sodium-deficient marmoset [3]
Doses: 3 mg/kg, 10 mg/kg Route of Administration: po (oral gavage); one time/day; 12-day Experimental Results: Plasma immunoreactive renin levels increased, blood pressure diminished, and Does not affect heart rate. There was no rebound increase in blood pressure after the end of aliskiren treatment at any dose. Inhibits RAS and controls the upregulation of pro-inflammatory cytokines. Animal/Disease Models: BALB/c mouse cancer cachexia model injected with C26 mouse colon cancer cells [4] Doses: 10 mg/kg Route of Administration: po (oral gavage); 5th day after C26 injection (as a preventive strategy, AP group) or day 12 (as treatment strategy, AT group); C26 20-day post-injection Experimental Results: Enhanced grip strength, coordination, and athletic ability. Suppresses serum Ang I and Ang II levels as well as serum and muscle tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels. |
| References |
[1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758
[2]. Ferri N, et al. Aliskiren inhibits prorenin-induced human aortic smooth muscle cell migration. J Renin Angiotensin Aldosterone Syst. 2015 Jun;16(2):284-91. [3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705. [4]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022. |
| Molecular Formula |
C30H53N3O6.HCL
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|---|---|
| Molecular Weight |
588.21926
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| CAS # |
173399-03-6
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| Related CAS # |
Aliskiren;173334-57-1;Aliskiren hemifumarate;173334-58-2;Aliskiren-d6 hydrochloride;1246815-96-2;Aliskiren fumarate;1196835-68-3;Aliskiren-d6 hemifumarate
|
| SMILES |
Cl.NC(CC(CC1C=CC(OC)=C(OCCCOC)C=1)C(C)C)C(O)CC(C(C)C)C(NCC(C)(C)C(N)=O)=O
|
| 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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7000 mL | 8.5002 mL | 17.0004 mL | |
| 5 mM | 0.3400 mL | 1.7000 mL | 3.4001 mL | |
| 10 mM | 0.1700 mL | 0.8500 mL | 1.7000 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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