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AMG-131, also known as INT-131, is a novel and potent selective PPARγ partial agonist and hypoglycemic agent. Possibly used to treat type 2 diabetes (T2DM).
| Targets |
PPARγ
|
|---|---|
| ln Vitro |
AMG131 (INT131) exhibits a Ki of approximately 10 nM when binding to PPARγ, displacing Rosiglitazone. Its affinity is approximately 20 times greater than that of either Rosiglitazone or Pioglitazone, and it has a selectivity of more than 1000 times for PPARγ over PPARα, PPARδ, or a group of other nuclear receptors. With no binding to PPARα or δ at 10 μM, 1000 times over the Ki for PPARγ, AMG131 exhibits high selectivity for PPARγ[1].
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| ln Vivo |
AMG131 (INT131; 80 mg/kg; 14-day oral treatment) improves glucose tolerance after in Zucker (fa/fa) rats following[2]
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| Animal Protocol |
Male Zucker fatty (fa/fa) rats ages 7-8 weeks[2]
80 mg/kg Administered once daily by oral gavage for 14 days |
| References | |
| Additional Infomation |
AMG-131 (T131), an orally-administered therapy, is expected to lower blood glucose in type II diabetic patients by improving the body’s ability to respond to insulin. T131 is a selective modulator of PPARg (peroxisome proliferator activated receptor gamma), a receptor involved in regulating the body’s ability to respond to insulin. T131 is not structurally related to the thiazolidinedione class of PPARg agonists, which includes Actos and Avandia.
Drug Indication Investigated for use/treatment in diabetes mellitus type 2. Mechanism of Action T131 is a selective modulator of PPARg (peroxisome proliferator activated receptor gamma), a receptor involved in regulating the body’s ability to respond to insulin. T131 is not structurally related to the thiazolidinedione class of PPARg agonists, which includes Actos and Avandia Pharmacodynamics T131, an orally-administered therapy, is expected to lower blood glucose in type II diabetic patients by improving the body’s ability to respond to insulin. T131 is not structurally related to the thiazolidinedione class of PPARg agonists, which includes Actos and Avandia |
| Molecular Formula |
C21H12CL4N2O3S
|
|---|---|
| Molecular Weight |
514.20858001709
|
| Exact Mass |
476
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| Elemental Analysis |
C, 49.05; H, 2.35; Cl, 27.58; N, 5.45; O, 9.33; S, 6.24
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| CAS # |
315224-26-1
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| Related CAS # |
849738-78-9 (besylate);315224-26-1;
|
| PubChem CID |
10229498
|
| Appearance |
White to light yellow solid powder
|
| LogP |
6.699
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
31
|
| Complexity |
697
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1=CC=C(S(NC2=CC(Cl)=C(OC3C=NC4=CC=CC=C4C=3)C(Cl)=C2)(=O)=O)C(Cl)=C1
|
| InChi Key |
NMRWDFUZLLQSBN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H12Cl4N2O3S/c22-13-5-6-20(16(23)8-13)31(28,29)27-14-9-17(24)21(18(25)10-14)30-15-7-12-3-1-2-4-19(12)26-11-15/h1-11,27H
|
| Chemical Name |
2,4-dichloro-N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)benzenesulfonamide
|
| Synonyms |
AMG-131; AMG131; AMG 131; INT-131; INT-131; NT-131; T-131; T-0903131; ibrigampar
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~250 mg/mL (~486.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9447 mL | 9.7237 mL | 19.4473 mL | |
| 5 mM | 0.3889 mL | 1.9447 mL | 3.8895 mL | |
| 10 mM | 0.1945 mL | 0.9724 mL | 1.9447 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02638038 | Completed | Drug: INT131 | Multiple Sclerosis, Relapsing Remitting | InteKrin Therapeutics, Inc. | February 2015 | Phase 2 |
| NCT00952445 | Completed | Drug: T0903131 Besylate Drug: Placebo |
Diabetes Mellitus, Type II | InteKrin Therapeutics, Inc. | December 2003 | Phase 2 |
| NCT00631007 | Completed | Drug: INT131 besylate Drug: Pioglitazone HCl |
Type 2 Diabetes Mellitus | InteKrin Therapeutics, Inc. | February 2008 | Phase 2 |
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