Size | Price | Stock | Qty |
---|---|---|---|
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
Other Sizes |
|
Purity: ≥98%
Atorvastatin Calcium (CI-981; CI981; Atorvastatin hemicalcium; liptonorm), an approved blockbuster drug of the statin class of LDL cholesterol-lowering/hypolipidemic medications, is a potent and selective inhibitor of HMG-CoA reductase with anti-hyperlipidemic effects. Atorvastatin isthe best-selling drug in the history of pharmaceuticals with a total of around US$130 billion for Pfizer during its 14 years on the market, making it the world's bestselling drug of all time. It acts by blocking the production of cholesterol. Atorvastatin is used primarily for lowering blood cholesterol and for prevention of events associated with cardiovascular disease.
ln Vitro |
After myocardial infarction, atorvastatin treatment reduces myocardial cell apoptosis by downregulating the expression of GRP78, caspase-12, and CHOP in myocardial cells. Additionally, heart failure and angiotensin II (Ang II) stimulation trigger endoplasmic reticulum (ER) stress[4].
|
---|---|
ln Vivo |
In the Ang II-induced ApoE-/- mice, atorvastatin (20–30 mg/kg; oral gavage; once daily; for 28 days; ApoE−/− mice) treatment dramatically reduces the amount of apoptotic cells, the activation of Caspase12 and Bax, and endoplasmic reticulum (ER) stress signaling proteins. After taking atorvastatin, proinflammatory cytokines like IL-6, IL-8, and IL-1β are all noticeably inhibited[5].
|
Animal Protocol |
Animal/Disease Models: Forty 8weeks old ApoE− /− mice induced with angiotensin II (Ang II)[5]
Doses: 20 mg/kg, 30 mg/kg Route of Administration: po (oral gavage); one time/day; for 28 days Experimental Results: Dramatically decreased ER stress signaling proteins, the number of apoptotic cells, and the activation of Caspase12 and Bax in the Ang II-induced ApoE−/− mice. Proinflammatory cytokines such as IL-6, IL-8, IL-1β were all remarkably 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. |
Molecular Formula |
2(C33H34FN2O5).CA
|
---|---|
Molecular Weight |
1155.34
|
CAS # |
134523-03-8
|
Related CAS # |
Atorvastatin;134523-00-5;Atorvastatin hemicalcium trihydrate;344920-08-7
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C1=C(C2C([H])=C([H])C([H])=C([H])C=2[H])C(C(N([H])C2C([H])=C([H])C([H])=C([H])C=2[H])=O)=C(C([H])(C([H])([H])[H])C([H])([H])[H])N1C([H])([H])C([H])([H])[C@]([H])(C([H])([H])[C@]([H])(C([H])([H])C(=O)O[H])O[H])O[H]
|
Synonyms |
Atorvastatin; CI 981; atorvastatin calcium trihydrate; atorvastatin, CI-981; CI981; Atorvastatin hemicalcium; calcium salt; trade name:liptonorm
|
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 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)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.33 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 (4.33 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. View More
Solubility in Formulation 3: 5% DMSO+castor oil:23 mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.8655 mL | 4.3277 mL | 8.6555 mL | |
5 mM | 0.1731 mL | 0.8655 mL | 1.7311 mL | |
10 mM | 0.0866 mL | 0.4328 mL | 0.8655 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05464628 | Completed | Drug: Atorvastatin Drug: ASC42 |
Healthy | Gannex Pharma Co., Ltd. | August 8, 2022 | Phase 1 |
NCT01645410 | Completed | Drug: Atorvastatin Calcium Tablets, 40 mg |
Healthy | Dr. Reddy's Laboratories Limited | March 2009 | Phase 1 |
NCT03247400 | Completed | Drug: 1% atorvastatin calcium salt ointment |
Non-segmental Vitiligo | Nicolaus Copernicus University | December 1, 2016 | Phase 1 Phase 2 |
NCT01555632 | Withdrawn | Drug: atorvastatin calcium Drug: placebo |
Recurrent Prostate Cancer Stage I Prostate Cancer |
University of Nebraska | March 2012 | Not Applicable |