| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| Other Sizes |
|
Purity: ≥98%
Atorvastatin (CI-981; CI981; Tozalip; Torvast; Cardyl; liptonorm) is an approved blockbuster drug of the statin class used as an LDL
cholesterol-lowering/hypolipidemic medication. It act as a potent and
selective inhibitor of HMG-CoA reductase.
| Targets |
HMG-CoA reductase
|
|---|---|
| ln Vitro |
By downregulating the expression of GRP78, caspase-12, and CHOP in cardiomyocytes during myocardial infarction, atorvastatin treatment lowers cardiomyocyte apoptosis. Additionally, it stimulates the endoplasmic reticulum (ER) in response to heart failure and angiotensin II (Ang II) stimulation. ) tension. 4].
|
| ln Vivo |
Treatment with atorvastatin (20–30 mg/kg; oral gavage; once daily; for 28 days; ApoE−/− mice) markedly decreased the amount of apoptotic cells, endoplasmic reticulum (ER) stress signaling proteins, and Caspase12 and Caspase12 activation. Bax in ApoE-/- mice triggered by Ang II. Following atorvastatin treatment, pro-inflammatory cytokines such IL-6, IL-8, and IL-1β were markedly suppressed [5].
|
| Enzyme Assay |
The HMG-CoA reductase assay kit from Sigma-Aldrich (St. Louis, MO, USA) with the catalytic domain of the human enzyme (recombinant GST fusion protein expressed in E. coli) was used, under conditions recommended by the manufacturer, to identify the most effective fraction of plant extract. The concentration of the purified human enzyme stock solution (Sigma) was 0.52–0.85 mg protein/mL. Reference statin drug pravastatin (from Sigma) was used as positive control. To characterize HMG-CoA reductase inhibition under defined assay conditions, reactions containing 4 μL of NADPH (to obtain a final concentration of 400 μM) and 12 μL of HMG-CoA substrate (to obtain a final concentration of 400 μM) in a final volume of 0.2 mL of 100 mM potassium phosphate buffer, pH 7.4 (containing 120 mM KCl, 1 mM EDTA, and 5 mM DTT), were initiated (time 0) by the addition of 2 μL of the catalytic domain of human recombinant HMG-CoA reductase and incubated in Eppendorf BioSpectrometer (equipped with thermostatically controlled cell holder) at 37°C in the presence or absence (control) of 1 μL aliquots of drugs dissolved in DMSO. The rates of NADPH consumed were monitored every 20 sec for up to 15 min by scanning spectrophotometrically [7].
|
| Cell Assay |
Cell proliferation assays were performed essentially as described previously. Briefly, SV-SMC from 5 different patients were seeded into 24-well cell culture plates at a density of 1 × 104 cells per well in full growth medium. Cells were incubated overnight and then quiesced in serum free medium for 3 days before transfer to full growth medium (10% FCS) containing 5 different statins at a range of concentrations. All statins were tested on cells from each individual patient. Medium and drugs were replaced after 2 days, and viable cell numbers were determined in triplicate wells after 4 days using Trypan Blue and a hemocytometer. The increase in cell number was calculated by subtracting the starting cell number (day 0) from the final cell number (day 4). Data were then normalized to control values (no statin) to correct for differences in proliferation rates between cells from different patients [2].
|
| Animal Protocol |
Animal/Disease Models: 40 8weeks old ApoE−/− mice, angiotensin II (Ang II) induced [5]
Doses: 20 mg/kg, 30 mg/kg Route of Administration: po (oral gavage); one time/day; continuous 28-day Experimental Results: Endoplasmic reticulum stress signaling proteins, the number of apoptotic cells, and the activation of Caspase12 and Bax were Dramatically diminished in Ang II-induced ApoE−/− mice. Pro-inflammatory cytokines such as IL-6, IL-8, and IL-1β were Dramatically inhibited. |
| References |
[1]. Santodomingo-Garzón T, et al. Atorvastatin inhibits inflammatory hypernociception. Br J Pharmacol. 2006 Sep;149(1):14-22.
[2]. Turner NA, et al. Comparison of the efficacies of five different statins on inhibition of human saphenous vein smooth muscle cell proliferation and invasion. J Cardiovasc Pharmacol. 2007 Oct;50(4):458-61. [3]. Nawrocki, J.W., et al., Reduction of LDL cholesterol by 25% to 60% in patients with primary hypercholesterolemia by atorvastatin, a new HMG-CoA reductase inhibitor. Arterioscler Thromb Vasc Biol, 1995. 15(5): p. 678-82. [4]. Song XJ, et al. Atorvastatin inhibits myocardial cell apoptosis in a rat model with post-myocardial infarction heart failure by downregulating ER stress response. Int J Med Sci. 2011;8(7):564-72. [5]. Li Y, et al. Inhibition of endoplasmic reticulum stress signaling pathway: A new mechanism of statins to suppress the development of abdominal aortic aneurysm. PLoS One. 2017 Apr 3;12(4):e0174821. [6]. Ming-Bai Hu, et al. Atorvastatin induces autophagy in MDA-MB-231 breast cancer cells. Ultrastruct Pathol. Sep-Oct 2018;42(5):409-415. [7]. In Vitro Screening for β-Hydroxy-β-methylglutaryl-CoA Reductase Inhibitory and Antioxidant Activity of Sequentially Extracted Fractions of Ficus palmata Forsk. Biomed Res Int. 2014; 2014: 762620. |
| Molecular Formula |
C33H35FN2O5
|
|---|---|
| Molecular Weight |
558.65
|
| Exact Mass |
558.253
|
| Elemental Analysis |
C, 70.95; H, 6.32; F, 3.40; N, 5.01; O, 14.32
|
| CAS # |
134523-00-5
|
| Related CAS # |
Atorvastatin hemicalcium salt;134523-03-8;(3S,5S)-Atorvastatin;501121-34-2;Atorvastatin-d5 hemicalcium;222412-82-0;(rel)-Atorvastatin;110862-48-1;Atorvastatin hemicalcium trihydrate;344920-08-7;Atorvastatin-d5 sodium;222412-87-5
|
| Appearance |
White to light yellow solid powder
|
| LogP |
5
|
| tPSA |
112A^2
|
| SMILES |
O=C(O)C[C@H](O)C[C@H](O)CCN1C(C2=CC=C(F)C=C2)=C(C3=CC=CC=C3)C(C(NC4=CC=CC=C4)=O)=C1C(C)C
|
| InChi Key |
XUKUURHRXDUEBC-KAYWLYCHSA-N
|
| InChi Code |
InChI=1S/C33H35FN2O5/c1-21(2)31-30(33(41)35-25-11-7-4-8-12-25)29(22-9-5-3-6-10-22)32(23-13-15-24(34)16-14-23)36(31)18-17-26(37)19-27(38)20-28(39)40/h3-16,21,26-27,37-38H,17-20H2,1-2H3,(H,35,41)(H,39,40)/t26-,27-/m1/s1
|
| Chemical Name |
(3R,5R)-7-(2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-3,5-dihydroxyheptanoic acid
|
| Synonyms |
CI-981 CI981 Atorvastatin liptonorm Lipilou Tozalip Torvast Cardyl
|
| HS Tariff Code |
2934.99.9001
|
| 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 (In Vitro) |
DMSO : ~50 mg/mL (~89.50 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7900 mL | 8.9501 mL | 17.9003 mL | |
| 5 mM | 0.3580 mL | 1.7900 mL | 3.5801 mL | |
| 10 mM | 0.1790 mL | 0.8950 mL | 1.7900 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA