Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Aliskiren hemifumarate (CGP-60536; CGP60536; Rasilez; SPP100; SPP-100; Tekturna), the hemifumarate salt form of Aliskiren, is a potent and direct renin inhibitor with antihypertensive activity. It inhibits renin with an IC50 of 1.5 nM. Aliskiren is the first-in-class drugs called direct renin inhibitors approved for use in the treatment of essential (primary) hypertension. Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin.
ln Vitro |
The in vitro inhibition of plasma renin activity (PRA) by isoskiren hemifumarate has IC50 values of 2.9 nM for human PRA and 8.0 nM for monkey PRA, respectively[1]. Human aortic smooth muscle cell migration induced by prorenin is inhibited by isoformisin hemifumarate (5 μM; 24 h)[2]. Aliskiren hemifumarate (1–10 μM; 24 h) significantly reduces prorenin-induced morphological alterations and lamellipodia development while having no effect on PDGF-BB activity[2].
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ln Vivo |
In marmosets with low sodium levels, isoproterenol (3 mg/kg, 10 mg/kg; po; daily; 0–12 d) inhibits renin and lowers blood pressure without altering heart rate[3]. Aliskiren hemifumarate (10 mg/kg; po; single dose) decreases tumor size, postpones the onset of cachexia, and increases the survival time of mice. Additionally, it increases locomotor activity, prevents muscular atrophy, and improves strength, mobility, and coordination throughout the entire body[4]. 20 days after C26 injection, a single dose of 10 mg/kg of aliskiren hemifumarate is administered po to alleviate oxidative stress linked to cancer cachexia[4].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: Smooth muscle cell (SMC) Tested Concentrations: 1-10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM. |
Animal Protocol |
Animal/Disease Models: Sodium-depleted marmosets[3]
Doses: 3 mg/kg, 10 mg/kg Route of Administration: po (oral gavage); one time/day; 12 days Experimental Results: Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate. demonstrated no rebound increase in BP following the end of treatment with either dose of aliskiren. Inhibited the RAS and controls the upregulation of pro‑inflammatory cytokines. Animal/Disease Models: Cancer cachexia model in balb/c (Bagg ALBino) mouse injected with C26 mouse colon carcinoma cells[4] Doses: 10 mg/kg Route of Administration: po (oral gavage); on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection Experimental Results: Enhanced grip strength, coordination, and locomotor activity. Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor‑α (TNF‑α) and inter‑ leukin‑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, 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. [5]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31. [6]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111(8), 1012-1018. |
Molecular Formula |
C30H53N3O6.1/2C4H4O4
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Molecular Weight |
609.83
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CAS # |
173334-58-2
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SMILES |
O=C(O)/C=C/C(O)=O.O=C(NCC(C)(C(N)=O)C)[C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)CC1=CC=C(OC)C(OCCCOC)=C1)N)O)C(C)C.O=C(NCC(C)(C(N)=O)C)[C@H](C(C)C)C[C@H](O)[C@@H](N)C[C@@H](C(C)C)CC2=CC=C(OC)C(OCCCOC)=C2
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InChi Key |
KLRSDBSKUSSCGU-KRQUFFFQSA-N
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InChi Code |
InChI=1S/2C30H53N3O6.C4H4O4/c2*1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36;5-3(6)1-2-4(7)8/h2*10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35);1-2H,(H,5,6)(H,7,8)
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Chemical Name |
(αS,γS,δS,ζS)-δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-benzeneoctanamide, 2E-butenedioate
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6398 mL | 8.1990 mL | 16.3980 mL | |
5 mM | 0.3280 mL | 1.6398 mL | 3.2796 mL | |
10 mM | 0.1640 mL | 0.8199 mL | 1.6398 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.