Catalog No.S2187

Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.

Price Stock Quantity  
USD 90 In stock
USD 70 In stock
USD 270 In stock
USD 770 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Avasimibe Chemical Structure

Avasimibe Chemical Structure
Molecular Weight: 501.72

Validation & Quality Control

1 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Avasimibe is available in the following compound libraries:

Product Information

  • Compare P450 (e.g. CYP17) Inhibitors
    Compare P450 (e.g. CYP17) Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.
Targets CYP2C9 [5] ACAT [1] CYP1A2 [5] CYP2C19 [5]
IC50 2.9 μM 3.3 μM 13.9 μM 26.5 μM
In vitro Avasimibe at concentration of 1μg/mL causes reduction of Total cholesterol (TC) and Esterified cholesterol (EC) through inhibiting LDL binding and decreasing scavenger receptor numbers during foam cell formation in human monocyte-derived macrophages (HMMs). Avasimibe at concentration of 2μg/mL enhances cholesterol efflux from established HMM foam cells preincubating with 10μg/ml LDL. [1] Avasimibe inhibits Lipoprotein(a) accumulation in the culture media of primary monkey hepatocyte in a dose-dependent manner with 11.9% -31.3% inhibition, the change is mainly associated with decreased ApoA. [2] Avasimibe incubating at concentration of 10 nM, 1 μM, and 10 μM for 24 hours in HepG2 cells reduce ApoB secretion into media by 25%, 27%, and 43%, respectively. Avasimibe decreases ApoB secretion by enhanced intracellular degradation of ApoB rather than decreased synthesis of ApoB. [3] Avasimibe inhibits ACTC with IC50 of 3.3 μM in IC-21 macrophages with consideration of the total inhibitor concentration in the assay sample. [4] Avasimibe inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively. [5] Avasimibe inhibits ACAT-1 expression and cholesterol ester synthesis in glioma cell lines. Avasimibe inhibits the growth of the glioma cells by inducing cell cycle arrest and apoptosis due to caspase-8 and caspase-3 activation. [6]
In vivo Avasimibe significantly reduces Lipoprotein(a) and total cholesterol levels in nine healthy male monkeys with a normal chow diet orally treated with CI-1011 at 30 mg/kg per day for 3 weeks, Lipoprotein(a) and total cholesterol levels reduce to 68 and 73% of control levels, respectively. Avasimibe decreases total cholesterol mainly due to reduction of low density lipoprotein (LDL). [2] Avasimibe decreases amyloid plaque load in the cortex and hippocampus and reduces the levels of insoluble Abeta40 and Abeta42 and C-terminal fragments of amyloid precursor protein (APP) in brain extracts in young human APP transgenic mice. Avasimibe reduces diffuse amyloid plaques by suppression of astrogliosis and enhanced microglial activation in aged human APP transgenic mice. [7]

Protocol(Only for Reference)

Kinase Assay: [1]

P450 Inhibition Studies Pooled human liver microsomes (HLM) from at least 15 donors are used for all inhibition assays. For IC50 determinations, the substrate probes are used at their approximate in vitro Km values. All incubations are performed with 100 mM potassium phosphate buffer (pH 7.4) and 1 mM NADPH. For CYP1A2 inhibition study, incubations are performed in a total volume of 0.5 ml, in duplicates with 0.1 mg/ml HLM, 30 μM phenacetin, 1 mM NADPH, and in the presence of avasimibe (0, 0.3, 0.75, 1.5, 3, 7.5, 15, 30, and 40 μM in 50 mM) in a potassium phosphate buffer at pH 7.4. After preincubation at 37 °C for 7 min, NADPH is added to initiate the enzyme reaction. The reaction mixture is quenched with 500 μl of ice-cold 100 ng/ml paracetamol-D4/CH3CN after 25 min. The standards (4-acetamidophenol, singlet) and quality controls (triplicates for low, medium, and high) are prepared at room temperature. After mixing, 0.2 ml of the samples is transferred to another plate and submitted for LC/MS/MS analysis after centrifugation at 3000 rpm for 10 min. A Supelco Discovery Amide C16, 100 × 2.1 mm (5-μm particle size) column (Supelco, Bellefonte, PA) is used. The mobile phase is isocratic, 40:60 [acetonitrile/formic acid, 0.1% (v/v)] at 0.2 ml/min.

Animal Study: [2]

Animal Models male cynomolgus monkeys
Formulation sterile 0.9% sodium chloride solution
Dosages 30 mg/kg
Administration Orally at a single dose per day for 3 weeks

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Lee HT, et al. J Med Chem, 1996, 39(26), 5031-5034.

[2] Ramharack R, et al. Atherosclerosis, 1998, 136(1), 79-87.

view more

Chemical Information

Download Avasimibe SDF
Molecular Weight (MW) 501.72


CAS No. 166518-60-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms CI-1011
Solubility (25°C) * In vitro DMSO 100 mg/mL (199.31 mM)
Ethanol 8 mg/mL (15.94 mM)
Water <1 mg/mL
In vivo 2% DMSO+corn oil 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate

Frequently Asked Questions

  • Question 1
    We want to use it for mice study by IP injection. I was wondering if you have any suggestions how to make a soluble solution for IP injection?

    Answer: S2187 Avasimibe can be dissolved in 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first, then add PEG and Tween. After they mixed well, then dilute with water. And we found after stayed for about 20min, the precipitation will go out. So please prepare the solution just before use.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related P450 (e.g. CYP17) Products

  • U73122

    U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN.

  • Liproxstatin-1

    Liproxstatin-1 is a potent ferroptosis inhibitor.

  • Epacadostat (INCB024360)

    Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.

  • Abiraterone Acetate

    Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.

    Features:Abiraterone is a drug used in castration-resistant prostate cancer.

  • Abiraterone

    Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.

    Features:Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.

  • Voriconazole

    Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.

  • Apigenin

    Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.

    Features:Much more potent than kaempferol and myricetin in CT-L inhibition.

  • Pioglitazone HCl

    Pioglitazone HCl is a selective peroxisome proliferator-activated receptor-gamma (PPARgamma) agonist, used to treat diabetes.

  • Itraconazole

    Itraconazole is a relatively potent inhibitor of CYP3A4, used as a triazole antifungal agent.

  • Fluconazole

    Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.

Recently Viewed Items

Tags: buy Avasimibe | Avasimibe supplier | purchase Avasimibe | Avasimibe cost | Avasimibe manufacturer | order Avasimibe | Avasimibe distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us