GNF4877
- CAS No.
- 2041073-22-5
- Chemical Name:
- GNF4877
- Synonyms
- GNF4877;CID 139600315;GNF-4877 GNF4877;CID 139600315(GNF-4877);3-Piperidinecarboxylic acid, 1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-, (3R)-;GNF 4877,GSK-3,inhibit,Glycogen synthase kinase-3,Glycogen synthase kinase 3,GNF-4877,GNF4877,Inhibitor,Dual specificity tyrosine regulated kinase,Dual specificity tyrosine phosphorylation regulated kinase,DYRK
- CBNumber:
- CB55540441
- Molecular Formula:
- C25H27FN6O4
- Molecular Weight:
- 494.52
- MDL Number:
- MFCD32263043
- MOL File:
- 2041073-22-5.mol
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
GNF4877 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2664 | GNF-4877 ≥98% (HPLC) | 2041073-22-5 | 5MG | $123 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML2664 | GNF-4877 ≥98% (HPLC) | 2041073-22-5 | 25MG | $396 | 2024-03-01 | Buy |
| ChemScene | CS-0105879 | GNF4877 98.85% | 2041073-22-5 | 5mg | $700 | 2021-12-16 | Buy |
| ChemScene | CS-0105879 | GNF4877 98.85% | 2041073-22-5 | 10mg | $1100 | 2021-12-16 | Buy |
| ChemScene | CS-0105879 | GNF4877 98.85% | 2041073-22-5 | 25mg | $2100 | 2021-12-16 | Buy |
GNF4877 Chemical Properties,Uses,Production
Biological Activity
GNF4877 is a potent inhibitor of DYRK1A and GSK3β with IC50 values of 6 nM and 16 nM, respectively, resulting in blocked NFATc nuclear export and increased β-cell proliferation (EC50 for mouse β (R7T1) cells 0.66 μM).
in vitro
High glucose concentrations and glucokinase activators (GKAs) increase Ca 2+ signalling in β-cells, and increase intracellular Ca 2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below the EC 50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca 2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca 2+ sup> channel activator) show additive activity with GNF4877.
in vivo
GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control.
| Animal Model: | Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto -DTA) 1 Gfi/J) with Doxycycline (28.8±2.4 g; 82±2 days) |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; twice a day; for 15 days |
| Result: | Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control. |
target
| GSK3β 16 nM (IC 50 ) | DYRK1A 6 nM (IC 50 ) |
GNF4877 Preparation Products And Raw materials
Raw materials
Preparation Products
GNF4877 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4182 | 55 | |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
| Chuzhou KeMail Chemical Technology Co., Ltd | 0550-5196001 15000891977 | wj520wjxby@126.com | China | 1836 | 55 |
| Luan lingxi Chemical Products Co., Ltd | 18712378369 | 690240416@qq.com | China | 282 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
| Chunchuang (Wuhan) Technology Co., Ltd | 15342225168 | yutianchun2007@126.com | China | 10006 | 58 |
| cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10011 | 58 |