| Identification | Back Directory | [Name]
INT-131 | [CAS]
315224-26-1 | [Synonyms]
INT-131
CHS 131
N-(3,5-DICHLORO-4-QUINOLIN-3-YLOXYPHENYL)-2,4-DIHYDROXYBENZENESULFONAMIDE
2,4-dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide
Benzenesulfonamide, 2,4-dichloro-N-[3,5-dichloro-4-(3-quinolinyloxy)phenyl]- | [Molecular Formula]
C21H12Cl4N2O3S | [MDL Number]
MFCD13152369 | [MOL File]
315224-26-1.mol | [Molecular Weight]
514.21 |
| Chemical Properties | Back Directory | [Boiling point ]
611.8±65.0 °C(Predicted) | [density ]
1.585±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (486.18 mM; Need ultrasonic) | [form ]
Solid | [pka]
5.30±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
AMG131 (INT131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM). AMG131 binds to PPARγ within the same binding pocket as the TZDs, but occupies a unique space in the pocket and contacts the receptor at distinct points from the TZDs. AMG131 is promising for research of type-2 diabetes mellitus[1][2][3]. | [Biological Activity]
INT131 is a brain penetrant, non-thiazolidinedione, highly potent and selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator (SPPARM) th at displays anti-diabetic activities. INT131 is a partial, rather than a full agonist of PPARγ, and in clinical trials has shown increased glucose tolerance without the weight gain and cardiovascular side effects seen with some of the full agonist. | [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. |
| [IC 50]
PPARγ | [storage]
Store at -20°C | [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. DOI:10.1155/2008/936906
[2] Alykhan Motani, et al. INT131: a selective modulator of PPAR gamma. J Mol Biol. 2009 Mar 13;386(5):1301-11. DOI:10.1016/j.jmb.2009.01.025
[3] Higgins LS, et al. The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer Insulin Sensitizer. PPAR Res. 2008;2008:936906. DOI:10.1155/2008/936906 |
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| Company Name: |
Struchem Co., Ltd.
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| Tel: |
0512-63009836 18994340901 |
| Website: |
www.beidapharma.com |
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