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| Targets |
SR1664 is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ). It binds to PPARγ and potently inhibits Cdk5-mediated phosphorylation of the receptor with an IC50 of 80 nM and a Ki of 28.67 nM. SR1664 does not exhibit PPARγ agonist activity. Its mechanism involves binding to PPARγ and blocking Cdk5-mediated phosphorylation, which is associated with antidiabetic effects.
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| ln Vitro |
F282 to alanine (F282A) mutation modifies the pharmacological impact of SR1664 (1uM; HEK293T cells) on PPARγ activity [1].
In vitro, SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation with an IC50 of 80 nM and a Ki of 28.67 nM. It does not exhibit PPARγ agonist activity. Its in vitro activity is characterized by potent and selective PPARγ inhibition without agonist activity. SR1664 has potential antidiabetic activity. |
| ln Vivo |
In vivo, SR1664 has potential antidiabetic activity. As a PPARγ inhibitor, it may modulate glucose metabolism and insulin sensitivity. However, detailed in vivo efficacy data for specific disease models are limited. SR1664 is primarily used as a research tool for studying PPARγ biology and diabetes.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SR1664 typically involve measuring its binding to PPARγ. The compound binds to PPARγ and inhibits Cdk5-mediated phosphorylation. These assays confirm its mechanism of action as a PPARγ inhibitor. Its lack of PPARγ agonist activity can also be confirmed using reporter gene assays.
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| Cell Assay |
In vitro cellular assays for SR1664 typically involve treating cells expressing PPARγ with the compound and measuring Cdk5-mediated PPARγ phosphorylation. SR1664 potently inhibits Cdk5-mediated PPARγ phosphorylation with an IC50 of 80 nM and a Ki of 28.67 nM. These cell-based studies demonstrate its functional inhibition of PPARγ phosphorylation without agonist activity.
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| Animal Protocol |
In vivo animal models for SR1664 may include models of diabetes or metabolic syndrome to evaluate its antidiabetic efficacy. The compound is administered by appropriate routes, and glucose metabolism and insulin sensitivity are assessed. However, detailed animal protocol information is limited. SR1664 is primarily used as a research tool for studying PPARγ biology and diabetes.
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| ADME/Pharmacokinetics |
SR1664 has a molecular weight of 547.6 and a molecular formula of C33H29N3O5. Its CAS number is 1338259-05-4. The compound is an antidiabetic agent that binds to PPARγ and inhibits Cdk5-mediated PPARγ phosphorylation with an IC50 of 80 nM and a Ki of 28.67 nM. SR1664 does not exhibit PPARγ agonist activity.
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| Toxicity/Toxicokinetics |
SR1664 is a PPARγ inhibitor with a well-characterized mechanism of action. As with any nuclear receptor modulator, potential toxicity may include effects on metabolism and inflammation. The compound's safety profile should be evaluated in preclinical toxicology studies. SR1664 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying PPARγ biology and diabetes.
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| References | |
| Additional Infomation |
[1,1'-Biphenyl]-2-carboxylic acid, 4'-[[2,3-Dimethyl-5-[[[(1s)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1h-indole-1-yl]methyl]- is an indolecarboxamide.
SR1664 (CAS# 1338259-05-4) is a potent and selective PPARγ inhibitor with potential antidiabetic activity. It binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation with an IC50 of 80 nM and a Ki of 28.67 nM. SR1664 does not exhibit PPARγ agonist activity. The compound is for research use only and not for human therapeutic use. |
| Molecular Formula |
C33H29N3O5
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|---|---|
| Molecular Weight |
547.61
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| Exact Mass |
547.21
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| CAS # |
1338259-05-4
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| PubChem CID |
53239854
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
828.8±65.0 °C at 760 mmHg
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| Flash Point |
455.0±34.3 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.648
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| LogP |
6.75
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
41
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| Complexity |
922
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=C(N(C2=C1C=C(C=C2)C(=O)N[C@@H](C)C3=CC=C(C=C3)[N+](=O)[O-])CC4=CC=C(C=C4)C5=CC=CC=C5C(=O)O)C
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| InChi Key |
IIJDFXNUWZTHIM-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C33H29N3O5/c1-20-22(3)35(19-23-8-10-25(11-9-23)28-6-4-5-7-29(28)33(38)39)31-17-14-26(18-30(20)31)32(37)34-21(2)24-12-15-27(16-13-24)36(40)41/h4-18,21H,19H2,1-3H3,(H,34,37)(H,38,39)/t21-/m0/s1
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| Chemical Name |
2-[4-[[2,3-dimethyl-5-[[(1S)-1-(4-nitrophenyl)ethyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acid
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| Synonyms |
SR 1664 SR-1664 SR1664
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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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~182.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 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 25.0 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: ≥ 2.5 mg/mL (4.57 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 25.0 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 | 1.8261 mL | 9.1306 mL | 18.2612 mL | |
| 5 mM | 0.3652 mL | 1.8261 mL | 3.6522 mL | |
| 10 mM | 0.1826 mL | 0.9131 mL | 1.8261 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.
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