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INT-131
CAS No. 315224-26-1
INT-131( AMG-131 | CHS 131 )
Catalog No. M24248 CAS No. 315224-26-1
INT-131, is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 78 | In Stock |
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| 5MG | 68 | In Stock |
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| 10MG | 116 | In Stock |
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| 25MG | 250 | In Stock |
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| 50MG | 398 | In Stock |
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| 100MG | 594 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameINT-131
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NoteResearch use only, not for human use.
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Brief DescriptionINT-131, is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator.
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DescriptionINT-131, is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator, which can be used for the treatment of type 2 diabetes mellitus (non-insulin dependent diabetes)(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.(In Vivo):AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following.
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In VitroAMG131 (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.
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In VivoAMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following Animal Model:Male Zucker fatty (fa/fa) rats ages 7-8 weeks 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.
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SynonymsAMG-131 | CHS 131
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PathwayMetabolic Enzyme/Protease
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TargetPPAR
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RecptorPPARγ
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Research Area——
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Indication——
Chemical Information
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CAS Number315224-26-1
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Formula Weight514.21
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Molecular FormulaC21H12Cl4N2O3S
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Purity>98% (HPLC)
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SolubilityDMSO:10 mM
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SMILESC1=CC=C2C(=C1)C=C(C=N2)OC3=C(C=C(C=C3Cl)NS(=O)(=O)C4=C(C=C(C=C4)Cl)Cl)Cl
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Kintscher U , Goebel M . INT-131, a PPARgamma agonist for the treatment of type 2 diabetes.[J]. Curr Opin Investig Drugs, 2009, 10(4):381-387.
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