AMG131

Modify Date: 2024-01-14 16:41:28

AMG131 Structure
AMG131 structure
 Common Name AMG131
CAS Number 315224-26-1 Molecular Weight 514.21
Density N/A Boiling Point N/A
Molecular Formula C21H12Cl4N2O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AMG131


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].

 Names

Name N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)-2,4-dihydroxybenzenesulfonamide
Synonym More Synonyms

 AMG131 Biological Activity

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
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.

 Chemical & Physical Properties

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

 Synthetic Route

3,5-dichloro-4-(quinolin-3-yloxy)-phenylamine structure

3,5-dichloro-4-...

CAS#:315228-24-1

2,4-Dichlorobenzenesulfonyl chloride structure

2,4-Dichloroben...

CAS#:16271-33-3

~%

AMG131 Structure

AMG131

CAS#:315224-26-1

Literature: WO2005/33074 A2, ; Page/Page column 33 ; WO 2005/033074 A2
3-(2,6-Dichloro-4-nitrophenoxy)quinoline structure

3-(2,6-Dichloro...

CAS#:315228-23-0

~%

AMG131 Structure

AMG131

CAS#:315224-26-1

Literature: Bioorganic and Medicinal Chemistry, , vol. 21, # 4 p. 979 - 992
1,2,3-Trichloro-5-nitrobenzene structure

1,2,3-Trichloro...

CAS#:20098-48-0

~%

AMG131 Structure

AMG131

CAS#:315224-26-1

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

 Synonyms

UNII-E7ILQ6U50J
AMG131
T-131 cpd
INT-131
T-131
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