| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Aliskiren D6 hemifumarate targets the same enzyme as its unlabeled parent drug. Aliskiren is a direct and orally active renin inhibitor with an IC50 of 1.5 nM. Renin is a key enzyme in the renin-angiotensin system that cleaves angiotensinogen to angiotensin I. By inhibiting renin, Aliskiren reduces the production of angiotensin II and aldosterone.
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| ln Vitro |
In vitro, plasma renin activity (PRA) is inhibited by isaliskiren hemifumarate, with an IC50 of 2.9 nM for human PRA and 8.0 nM for monkey PRA [1]. Human aortic smooth muscle cell migration mediated by prorenin is inhibited by isoformaliskiren hemifumarate (5 μM; 24 h) [2]. Aliskiren hemifumarate (1–10 μM; 24 hours) has no discernible effect on PDGF-BB activity, but it suppresses the development of lamellipodia and morphological alterations generated by prorenin [2].
Aliskiren D6 hemifumarate is primarily used as an analytical internal standard rather than for its pharmacological activity. Aliskiren hemifumarate is a direct and orally active renin inhibitor. The compound is used in LC-MS/MS methods for the quantification of Aliskiren in biological matrices. The deuterium labeling provides a mass shift for accurate quantification. |
| ln Vivo |
In sodium-depleted marmosets, aliskiren hemifumarate (3 mg/kg, 10 mg/kg; oral; daily; 0–12 days) suppresses renin and reduces blood pressure without changing heart rate [3]. In mice, aliskiren hemifumarate (10 mg/kg; oral; single dosage) decreases tumors, postpones the onset of cachexia, and increases survival. Moreover, it can boost physical activity, prevent muscle atrophy, and increase general body strength, mobility, and coordination [4]. Twenty days following a C26 injection, a single oral dosage of 10 mg/kg of aliskiren hemifumarate is administered to alleviate oxidative stress linked to cancer cachexia [4].
Aliskiren (10 and 30 mg/kg per day) reduces blood pressure and prevents albuminuria in vivo. Aliskiren D6 hemifumarate serves as a critical tool in pharmacokinetic studies to accurately track drug absorption, distribution, metabolism, and excretion. It has been used in bioequivalence studies and method validation for regulatory submissions. |
| Enzyme Assay |
In vitro enzyme assays for Aliskiren D6 hemifumarate are typically performed as part of analytical method validation. The compound is used as an internal standard in LC-MS/MS assays for the quantification of Aliskiren. It is dissolved in an appropriate solvent and spiked into biological matrices at known concentrations. Calibration curves are generated by plotting the peak area ratio of Aliskiren to Aliskiren D6 against the concentration of Aliskiren.
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| Cell Assay |
Cell Viability 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. For in vitro cell-based assays, Aliskiren D6 hemifumarate can be used in studies investigating Aliskiren's cellular effects, though its primary use is as an analytical internal standard. Cells relevant to the renin-angiotensin system can be treated with the compound. However, due to its role as an internal standard, it is more frequently used in analytical quantification. |
| 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. In vivo animal studies with Aliskiren D6 hemifumarate are primarily pharmacokinetic. The compound is administered orally to rodents, and blood samples are collected at predetermined time points. Plasma concentrations of both labeled and unlabeled Aliskiren are analyzed by LC-MS/MS using Aliskiren D6 as the internal standard. Pharmacodynamic effects, such as blood pressure reduction, can be evaluated. |
| ADME/Pharmacokinetics |
Aliskiren D6 hemifumarate has a molecular weight of 1231.66 g/mol. Synonyms: CGP 60536 D6 hemifumarate, SPP 100 D6 hemifumarate, Rasilez D6, Tekturna D6. Storage: powder at -20°C. Solubility: DMSO. The compound is a hexa-deuterated stable isotope-labeled form of Aliskiren hemifumarate.
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| Toxicity/Toxicokinetics |
As a deuterium-labeled analog of an approved antihypertensive drug, Aliskiren D6 hemifumarate is expected to have a similar toxicity profile to Aliskiren, though toxicity studies are typically not performed on the labeled compound. Aliskiren is generally well-tolerated, with common side effects including diarrhea, headache, and nasopharyngitis. The compound is used in very small quantities as an analytical internal standard.
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| References |
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| Additional Infomation |
Alisartan fumarate is the hemifumarate of alisartan, an antihypertensive drug. It contains the alisartan molecule. Alisartan fumarate is an orally effective non-peptide renin inhibitor with antihypertensive activity. Alisartan selectively binds to the S3 subpocket of renin. Renin is an enzyme in the renin-angiotensin-aldosterone system (RAAS) responsible for converting angiotensinogen to angiotensin I (AT1). By inhibiting renin activity, the conversion of angiotensinogen to angiotensin I is prevented, which in turn prevents the conversion of angiotensin I to angiotensin II. This prevents arterial vasoconstriction caused by angiotensin II and inhibits aldosterone production from angiotensin II. Since aldosterone causes sodium and water reabsorption, ultimately leading to an increase in extracellular fluid volume, alisartan can prevent these effects that lead to increased blood pressure. See also: Alisartan (contains the active ingredient); Alisartan fumarate; Amlodipine besylate (one of the ingredients); Alisartan fumarate; Hydrochlorothiazide (one of the ingredients)... See more...
Aliskiren D6 hemifumarate is a deuterium-labeled form of Aliskiren hemifumarate, a direct and orally active renin inhibitor. Aliskiren has an IC50 of 0.6-1.5 nM for the human enzyme. It is approved as an antihypertensive drug (Rasilez, Tekturna). The labeled compound is used as an internal standard for analytical and pharmacokinetic studies. It is not intended for therapeutic use. |
| Molecular Formula |
C64H110N6O16
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|---|---|
| Molecular Weight |
1231.7
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| Exact Mass |
1218.8
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| Related CAS # |
Aliskiren;173334-57-1;Aliskiren hydrochloride;173399-03-6;Aliskiren-d6 hydrochloride;1246815-96-2;Aliskiren-d6 hemifumarate
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| PubChem CID |
6918427
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| Appearance |
White to off-white solid powder
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| Melting Point |
72-75?C
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| Vapour Pressure |
1.59E-23mmHg at 25°C
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| LogP |
9.881
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
40
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| Heavy Atom Count |
86
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| Complexity |
836
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| Defined Atom Stereocenter Count |
8
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| SMILES |
[2H]C([2H])([2H])C([C@H](C[C@@H]([C@H](C[C@H](CC1=CC(=C(C=C1)OC)OCCCOC)C(C)C)N)O)C(=O)NCC(C)(C)C(=O)N)C([2H])([2H])[2H].[2H]C([2H])([2H])OCCCOC1=C(C=CC(=C1)C[C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N)C(C)C)OC([2H])([2H])[2H].C(=C/C(=O)O)\C(=O)O
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| InChi Key |
KLRSDBSKUSSCGU-PFGUTONBSA-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)/b;;2-1+/t2*22-,23-,24-,25-;/m00./s1/i7D3,8D3;3D3,4D3;
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| Chemical Name |
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-2-(1,1,1,3,3,3-hexadeuteriopropan-2-yl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methylnonanamide;(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-8-methyl-2-propan-2-yl-7-[[4-(trideuteriomethoxy)-3-[3-(trideuteriomethoxy)propoxy]phenyl]methyl]nonanamide;(E)-but-2-enedioic 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) |
H2O : ≥ 50 mg/mL (~41.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (41.00 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8119 mL | 4.0594 mL | 8.1189 mL | |
| 5 mM | 0.1624 mL | 0.8119 mL | 1.6238 mL | |
| 10 mM | 0.0812 mL | 0.4059 mL | 0.8119 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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