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AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a K i of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM) In Vitro AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a K i 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 K i for PPARγ. 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 followingMCE 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 weeksDosage: 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. Form:Solid IC50& Target:PPARγ
中文名称
AMG131, 过氧化物酶体增殖激活受体伽马调节剂
英文名称
AMG131
中文别名
-
英文别名
CHS-131 | Q27276976 | SCHEMBL634767 | 2,4-DICHLORO-N-(3,5-DICHLORO-4-((QUINOLIN-3- YL)OXY)PHENYL)BENZENE-1-SULFONAMIDE | DB05490 | T-131 | 2,4-dichloro-N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)benzenesulfonamide | 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-
CAS号
315224-26-1
分子式
C21H12Cl4N2O3S
分子量
514.21 g/mol
精确质量
≥99%
PSA
76.700 Ų
Logp
6.8
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AMG131, 过氧化物酶体增殖激活受体伽马调节剂 5mg

品牌:阿拉丁
货号:A651398-5mg
级别: ≥99%
货期:30天
已售 566 件
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