ChemicalBook > CAS DataBase List > N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

Product Name
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
CAS No.
864082-47-3
Chemical Name
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
Synonyms
CS-557;RHO-15;GSK 429286 A;RHO-15(GSK429286A);GSK429286A (DMSO solution);GSK 429286A;GSK-429286A;RHO-15;GSK429286A;GSK-429286A;GSK 429286A;N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)-phenyl)-1,4,5,6-tetrahydrop;N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide;N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
CBNumber
CB12484722
Molecular Formula
C21H16F4N4O2
Formula Weight
432.37
MOL File
864082-47-3.mol
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N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Property

Boiling point:
688.4±55.0 °C(Predicted)
Density 
1.468
storage temp. 
Sealed in dry,2-8°C
solubility 
DMSO: ≥10mg/mL
pka
12.10±0.40(Predicted)
form 
powder
color 
white to beige
CAS DataBase Reference
864082-47-3
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Safety

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
15262
Product name
GSK429286A
Purity
≥98%
Packaging
1mg
Price
$34
Updated
2024/03/01
Cayman Chemical
Product number
15262
Product name
GSK429286A
Purity
≥98%
Packaging
5mg
Price
$109
Updated
2024/03/01
Cayman Chemical
Product number
15262
Product name
GSK429286A
Purity
≥98%
Packaging
10mg
Price
$198
Updated
2024/03/01
ChemScene
Product number
CS-0095
Product name
GSK429286A
Purity
98.75%
Packaging
50mg
Price
$260
Updated
2021/12/16
AK Scientific
Product number
SYN1071
Product name
GSK429286A
Packaging
1mg
Price
$110
Updated
2021/12/16
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N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Chemical Properties,Usage,Production

Uses

GSK 429286 is a selective Rho-kinase (ROCK) inhibitor.It is orally available and has been shown to dramatically reduce mean arterial pressure in spontaneously hypertensive rats.

Definition

ChEBI: N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide is a member of (trifluoromethyl)benzenes.

Biological Activity

gsk429286a is a selective inhibitor of rock1 and rock2 with ic50 value of 14 nm and 63 nm, respectively [1].rho-kinase (rock) is a member of agc (protein kinase a, protein kinase g and protein kinase c) family and plays an important role in promoting actin-myosin-mediated contractile force generation [2].gsk429286a is a potent rock inhibitor and has a different activity with the reported rock inhibitor y27632. using gst method, it is shown that gsk429286a treatment (10 μm) increased mypt phosphrylation at thr850 via inhibiting rock which mediated this phosphorylation process [3].in male sprague-dawley rat model with spontaneously hypertensive, oral administration of gsk429286a (30 mg/kg) marks reduced mean arterial pressure and the maximum decreased was as 50 mmhg after nearly 2 h treatment [4].

storage

+4°C

References

[1]. nichols, r.j., et al., substrate specificity and inhibitors of lrrk2, a protein kinase mutated in parkinson's disease. biochem j, 2009. 424(1): p. 47-60.
[2]. shi, j., et al., distinct roles for rock1 and rock2 in the regulation of cell detachment. cell death dis, 2013. 4: p. e483.
[3]. davis, d.a., et al., increased therapeutic potential of an experimental anti-mitotic inhibitor sb715992 by genistein in pc-3 human prostate cancer cell line. bmc cancer, 2006. 6: p. 22.
[4]. goodman, k.b., et al., development of dihydropyridone indazole amides as selective rho-kinase inhibitors. j med chem, 2007. 50(1): p. 6-9.

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide manufacturers

Career Henan Chemical Co
Product
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide 864082-47-3
Price
US $9.80/KG
Min. Order
1g
Purity
≥99%
Supply Ability
100kg
Release date
2019-12-24

864082-47-3, N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamideRelated Search:


  • RHO-15(GSK429286A)
  • GSK 429286 A
  • RHO-15
  • N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide
  • GSK 429286 A N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide GSK 429286 A
  • N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)-phenyl)-1,4,5,6-tetrahydrop
  • N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide
  • CS-557
  • GSK429286A;GSK-429286A;GSK 429286A
  • GSK 429286A;GSK-429286A;RHO-15
  • 3-Pyridinecarboxamide, N-(6-fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide USP/EP/BP
  • GSK429286A (DMSO solution)
  • 864082-47-3
  • Inhibitors