1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. A 922500

A 922500 (Synonyms: DGAT-1 Inhibitor 4a)

Cat. No.: HY-10038 Purity: 98.50%
Handling Instructions

A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.

For research use only. We do not sell to patients.

A 922500 Chemical Structure

A 922500 Chemical Structure

CAS No. : 959122-11-3

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 139 In-stock
Estimated Time of Arrival: December 31
5 mg USD 126 In-stock
Estimated Time of Arrival: December 31
10 mg USD 176 In-stock
Estimated Time of Arrival: December 31
50 mg USD 563 In-stock
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100 mg USD 840 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    A 922500 purchased from MCE. Usage Cited in: Nat Commun. 2020 Jun 11;11(1):2967.

    The spatiotemporal distribution of LD is analyzed 5 dpi by immunofluorescence. Compared to DMSO control, cells treated with A922500 (DGAT1i) harbor only scarce LDs. Both the number and average volume of LDs are significantly reduced in the presence of DGAT1i.

    A 922500 purchased from MCE. Usage Cited in: Cell Metab. 2020 Aug 4;32(2):229-242.e8.

    Effects of Butyrate (But, 1 mM), Valproate (Vpa, 5 mM) and Vorinostat (Vor, 1 μM) on the expression of P-gp and BCRP, NF-кB p65 and phosphorylated p65 (p-p65), and IкBα and phosphorylated IкBα (p-IкBα).

    A 922500 purchased from MCE. Usage Cited in: Cell Metab. 2020 Aug 4;32(2):229-242.e8.

    Representative fluorescence imaging and quantification of ROS in U251 cells treated with DGAT1 inhibitor A-922500 (20 mg/mL) for 24 h or shRNA for 48 h in the presence or absence of the CPT1 inhibitor Etomoxir (ETO, 6 mM).

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    Description

    A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.

    IC50 & Target

    IC50: 9 nM (human DGAT-1), 22 nM (mouse DGAT-1)[1]

    In Vitro

    A 922500 (A-922500) demonstrates excellent selectivity over other acyltransferases, including DGAT-2 (IC50=53 μM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50=296 μM) [1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    428.48

    Formula

    C₂₆H₂₄N₂O₄

    CAS No.

    959122-11-3

    SMILES

    O=C(NC1=CC=C(C2=CC=C(C([[email protected]@H]3CCC[[email protected]]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (116.69 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3338 mL 11.6692 mL 23.3383 mL
    5 mM 0.4668 mL 2.3338 mL 4.6677 mL
    10 mM 0.2334 mL 1.1669 mL 2.3338 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [1]

    Mice and Hamsters[1]
    Thirteen-week-old male Golden Syrian hamsters (n=40), initially weighing approximately 140 g, are used. Ten-week-old Male Zucker fatty rats (n=32), weighing between 270 and 330 g, are used. After collection of baseline lipid profiles, hyperlipidemic hamsters (n=10/group) and Zucker fatty rats (n=8/group) are administered vehicle [20:80 (v/v), polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v)] or DGAT-1 inhibitor A 922500 (A-922500) at 0.03, 0.3, and 3 mg/kg, once daily by oral gavage. The dosing volume is 5 mL/kg. Serum lipid profiles are then measured 3 h after the dose on day 7 and day 14. Hamsters continue to be fed a high-fat diet with 10% fructose in the drinking water throughout the treatment period. Zucker fatty rats remain on standard rodent diet throughout the study.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 98.50%

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    Keywords:

    A 922500DGAT-1 Inhibitor 4aA922500A-922500AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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    Product Name:
    A 922500
    Cat. No.:
    HY-10038
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