ChemicalBook > CAS DataBase List > GNF4877

GNF4877

Product Name
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
Formula Weight
494.52
MOL File
2041073-22-5.mol
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GNF4877 Property

Boiling point:
669.7±55.0 °C(Predicted)
Density 
1.367±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: 4.17 mg/mL (8.43 mM and warming)
pka
2.82±0.70(Predicted)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2664
Product name
GNF-4877
Purity
≥98% (HPLC)
Packaging
5MG
Price
$123
Updated
2024/03/01
Sigma-Aldrich
Product number
SML2664
Product name
GNF-4877
Purity
≥98% (HPLC)
Packaging
25MG
Price
$396
Updated
2024/03/01
ChemScene
Product number
CS-0105879
Product name
GNF4877
Purity
98.85%
Packaging
5mg
Price
$700
Updated
2021/12/16
ChemScene
Product number
CS-0105879
Product name
GNF4877
Purity
98.85%
Packaging
10mg
Price
$1100
Updated
2021/12/16
ChemScene
Product number
CS-0105879
Product name
GNF4877
Purity
98.85%
Packaging
25mg
Price
$2100
Updated
2021/12/16
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GNF4877 Chemical Properties,Usage,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

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GNF4877 Suppliers

China 21 United States 2 Global 23
DC Chemicals
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021-58447131 13564518121
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sales@dcchemicals.com
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China
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
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+86-21-52996696
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China
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ShangHai Biochempartner Co.,Ltd
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17754423994 17754423994
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2853530910@QQ.com
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Chuzhou KeMail Chemical Technology Co., Ltd
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0550-5196001 15000891977
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0550-5196001
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wj520wjxby@126.com
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China
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Luan lingxi Chemical Products Co., Ltd
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18712378369
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690240416@qq.com
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China
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Zhejiang J&C Biological Technology Co.,Limited
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+1-2135480471 +1-2135480471
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sales@sarms4muscle.com
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China
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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QQ 3610331285
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sales@chemegen.com
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China
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Chunchuang (Wuhan) Technology Co., Ltd
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15342225168
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yutianchun2007@126.com
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cjbscvictory
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Shanghai Sunway Pharmaceutical Technology Co.,Ltd.
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021-51816796-820 13611835272
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sales2@sunwaypharm.com
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China
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Zhengzhou convergence chemical co., LTD
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0371-0371-55153829 18003835034
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18003835034（微信）
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Beijing Jin Ming Biotechnology Co., Ltd.
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010-60605840
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China
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Hubei Kele Fine Chemical Co., Ltd
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Bide Pharmatech Ltd.
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Wuhan Yingnuo Pharmaceutical Technology Co., Ltd.
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TargetMol Chemicals Inc.
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Nantong QuanYi Biotechnology Co., Ltd
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Shanghai Jieshikai Biotechnology Co. , Ltd.
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021-57520305 15221441005
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RD International Technology Co., Limited
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Olix (Shanghai) Pharmaceutical Technology Co., Ltd
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Shanghai Hao Zhun Biological Technology Co., Ltd.
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2041073-22-5, GNF4877Related Search:


  • GNF4877
  • CID 139600315
  • 3-Piperidinecarboxylic acid, 1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-, (3R)-
  • CID 139600315(GNF-4877)
  • 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
  • GNF-4877 GNF4877
  • 2041073-22-5