315224-26-1

315224-26-1 structure

Name: AMG131
Chemical Name: N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)-2,4-dihydroxybenzenesulfonamide
CAS Number: 315224-26-1
Molecular Formula: C₂₁H₁₂Cl₄N₂O₃S
Molecular Weight: 514.21
Catalog: Signaling Pathways Cell Cycle/DNA Damage PPAR
Create Date: 2018-12-29 18:12:37
Modify Date: 2024-01-14 16:41:28
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].

Name	N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)-2,4-dihydroxybenzenesulfonamide
Synonyms	UNII-E7ILQ6U50J AMG131 T-131 cpd INT-131 T-131

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].
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR Research Areas >> Metabolic Disease
Target	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].
In Vivo	AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following[2] 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.
References	[1]. Linda S Higgins,et al. The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer Insulin Sensitizer. PPAR Res. 2008;2008:936906. [2]. Alykhan Motani, et al. INT131: a selective modulator of PPAR gamma. J Mol Biol. 2009 Mar 13;386(5):1301-11.

Molecular Formula	C₂₁H₁₂Cl₄N₂O₃S
Molecular Weight	514.21
Exact Mass	476.00000
PSA	117.13000
LogP	6.69970
Storage condition	-20°C

315228-24-1

16271-33-3

315224-26-1

Literature: WO2005/33074 A2, ; Page/Page column 33 ; WO 2005/033074 A2

315228-23-0

315224-26-1

Literature: Bioorganic and Medicinal Chemistry, , vol. 21, # 4 p. 979 - 992

20098-48-0

315224-26-1

Literature: Bioorganic and Medicinal Chemistry, , vol. 21, # 4 p. 979 - 992

Precursor 4
315228-24-1 16271-33-3 315228-23-0 20098-48-0
DownStream 0

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