Lotiglipron
Based on 1 Customer Validation
Lotiglipron (PF-07081532) is an orally active GLP-1R agonist. Lotiglipron reduces glucose and body weight, and can be used for research of Type 2 diabetes mellitus (T2DM).
For research use only. We do not sell to patients.
- Purity : 98.96%
- CAS No.: 2401892-75-7
- Formula: C31H31ClN4O5
- Molecular Weight:575.05
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
In Vitro
Lotiglipron exhibits moderate affinity to GLP-1R, Ki for mutated rat GLP-1R S33W is 2770 nM. Lotiglipron promotes the cAMP accumulation (EC50 on the high-density expressed mutant rat GLP-1R S33W is 26.9 nM), stimulates β-arrestin 1/2 recruitment (EC50 on the mutant rat GLP-1R S33W is 198 nM and 274 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2401892-75-7
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Appearance Solid
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Molecular Weight 575.05
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Formula C31H31ClN4O5
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Color White to off-white
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SMILES
C[C@@]1(C2=CC=C(C=N2)Cl)OC3=C(C4CCN(CC4)CC(N(C5=C6)C[C@@H]7CCO7)=NC5=CC=C6C(O)=O)C=CC=C3O1
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Synonyms
PF-07081532
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (217.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7390 mL | 8.6949 mL | 17.3898 mL | 43.4745 mL |
| 5 mM | 0.3478 mL | 1.7390 mL | 3.4780 mL | 8.6949 mL | |
| 10 mM | 0.1739 mL | 0.8695 mL | 1.7390 mL | 4.3474 mL | |
| 15 mM | 0.1159 mL | 0.5797 mL | 1.1593 mL | 2.8983 mL | |
| 20 mM | 0.0869 mL | 0.4347 mL | 0.8695 mL | 2.1737 mL | |
| 25 mM | 0.0696 mL | 0.3478 mL | 0.6956 mL | 1.7390 mL | |
| 30 mM | 0.0580 mL | 0.2898 mL | 0.5797 mL | 1.4491 mL | |
| 40 mM | 0.0435 mL | 0.2174 mL | 0.4347 mL | 1.0869 mL | |
| 50 mM | 0.0348 mL | 0.1739 mL | 0.3478 mL | 0.8695 mL | |
| 60 mM | 0.0290 mL | 0.1449 mL | 0.2898 mL | 0.7246 mL | |
| 80 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5434 mL | |
| 100 mM | 0.0174 mL | 0.0869 mL | 0.1739 mL | 0.4347 mL |