Aliskiren Hemifumarate (CGP 60536)

Alias:
Cat No.:V1771 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.
Aliskiren Hemifumarate (CGP 60536) Chemical Structure CAS No.: 173334-58-2
Product category: RAAS
This product is for research use only, not for human use. We do not sell to patients.
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25mg
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Other Forms of Aliskiren Hemifumarate (CGP 60536):

  • Aliskiren (CGP 60536)
  • Aliskiren HCl
  • Aliskiren D6 Hydrochloride
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
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].
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H53N3O6.1/2C4H4O4
Molecular Weight
609.83
CAS #
173334-58-2
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
InChi Key
KLRSDBSKUSSCGU-KRQUFFFQSA-N
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)
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
Synonyms

CGP060536B; SPP-100;CGP 060536B; SPP 100;CGP-060536B; Rasilez; SPP100; Tekturna

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 Data
Solubility (In Vitro)
DMSO: 100 mg/mL (164.0 mM)
Water:100 mg/mL (164.0 mM)
Ethanol:100 mg/mL (164.0 mM)
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.

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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.

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