GS-9667
Based on 1 Customer Validation
GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.08%
- CAS. Nr.: 618380-90-8
- Formel: C21H24FN5O4S
- Molecular Weight:461.51
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
Beschreibung
Chemical Information
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CAS. Nr. 618380-90-8
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Appearance Solid
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Molecular Weight 461.51
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Formel C21H24FN5O4S
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Color Light yellow to yellow
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SMILES
O[C@H]1[C@@H](O[C@@H]([C@H]1O)CSC2=C(C=CC=C2)F)N3C4=NC=NC(N[C@H]5[C@@H](CCC5)O)=C4N=C3
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Synonyms
CVT 3619
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (270.85 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Large-size fat particle sorting
Large-size fat particle sorting is widely used to isolate cells up to 200 μm in diameter. Single-cell flow sorting will allow greater insight into adipocyte heterogeneity by identifying gene expression, protein composition, and metabolic signatures at the single-cell level.
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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
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Marjan Fatholahi, et al. A novel partial agonist of the A(1)-adenosine receptor and evidence of receptor homogeneity in adipocytes. J Pharmacol Exp Ther. 2006 May;317(2):676-84. [Content Brief]
[2]. Peter M Staehr, et al. Reduction of free fatty acids, safety, and pharmacokinetics of oral GS-9667, an A(1) adenosine receptor partial agonist. J Clin Pharmacol. 2013 Apr;53(4):385-92. [Content Brief]
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 | 2.1668 mL | 10.8340 mL | 21.6680 mL | 54.1700 mL |
| 5 mM | 0.4334 mL | 2.1668 mL | 4.3336 mL | 10.8340 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1668 mL | 5.4170 mL | |
| 15 mM | 0.1445 mL | 0.7223 mL | 1.4445 mL | 3.6113 mL | |
| 20 mM | 0.1083 mL | 0.5417 mL | 1.0834 mL | 2.7085 mL | |
| 25 mM | 0.0867 mL | 0.4334 mL | 0.8667 mL | 2.1668 mL | |
| 30 mM | 0.0722 mL | 0.3611 mL | 0.7223 mL | 1.8057 mL | |
| 40 mM | 0.0542 mL | 0.2709 mL | 0.5417 mL | 1.3543 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0834 mL | |
| 60 mM | 0.0361 mL | 0.1806 mL | 0.3611 mL | 0.9028 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2709 mL | 0.6771 mL | |
| 100 mM | 0.0217 mL | 0.1083 mL | 0.2167 mL | 0.5417 mL |