1. Cell Cycle/DNA Damage
  2. PPAR
  3. AMG131

AMG131 (Synonyms: INT131)

Cat. No.: HY-117103 Purity: 99.13%
Handling Instructions

AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM).

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

AMG131 Chemical Structure

AMG131 Chemical Structure

CAS No. : 315224-26-1

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5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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Description

AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)[1][2].

IC50 & Target[1][2]

PPARγ

 

In Vitro

AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM, demonstrating ~20-fold higher affinity than either Rosiglitazone or Pioglitazone, and with greater than 1000-fold selectivity for PPARγ over PPARα, PPARδ, or a set of other nuclear receptors. AMG131 is highly selective for PPARγ, with no binding to PPARα or δ at 10 μM, 1000 fold over the Ki for PPARγ[1].

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

In Vivo

AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following[2]

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

Animal Model: Male Zucker fatty (fa/fa) rats ages 7-8 weeks[2]
Dosage: 80 mg/kg
Administration: Administered once daily by oral gavage for 14 days
Result: Exhibited maximal efficacy comparable to that of Rosiglitazone with respect to plasma glucose clearance in an oral glucose tolerance test. Reduced baseline insulin levels, similar to Rosiglitazone, could improve insulin sensitivity in treated animals.
Molecular Weight

514.21

Formula

C₂₁H₁₂Cl₄N₂O₃S

CAS No.
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 : 250 mg/mL (486.18 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9447 mL 9.7237 mL 19.4473 mL
5 mM 0.3889 mL 1.9447 mL 3.8895 mL
10 mM 0.1945 mL 0.9724 mL 1.9447 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: ≥ 2.08 mg/mL (4.05 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
AMG131
Cat. No.:
HY-117103
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