ChemicalBook > CAS DataBase List > AMG-333

AMG-333

Product Name
AMG-333
CAS No.
1416799-28-4
Chemical Name
AMG-333
Synonyms
AMG-333;AMG333;AMG 333;AMG-333 ,S6638;AMG 333, 10 mM in DMSO;Inhibitor,AMG333,TRP Channel,inhibit,Transient receptor potential channels,AMG 333;(S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid;3-Pyridinecarboxylic acid, 6-[[[(S)-(3-fluoro-2-pyridinyl)[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]amino]carbonyl]-
CBNumber
CB64667528
Molecular Formula
C20H12F5N3O4
Formula Weight
453.32
MOL File
1416799-28-4.mol
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AMG-333 Property

storage temp. 
Store at -20°C
solubility 
DMSO : ≥ 125 mg/mL (275.74 mM)
form 
A solid
color 
White to off-white
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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.

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

Tocris
Product number
6874
Product name
AMG333
Purity
≥98%(HPLC)
Packaging
50
Price
$715
Updated
2021/12/16
ChemScene
Product number
CS-0062825
Product name
AMG333
Purity
99.76%
Packaging
5mg
Price
$100
Updated
2021/12/16
ChemScene
Product number
CS-0062825
Product name
AMG333
Purity
99.76%
Packaging
10mg
Price
$160
Updated
2021/12/16
ChemScene
Product number
CS-0062825
Product name
AMG333
Purity
99.76%
Packaging
25mg
Price
$380
Updated
2021/12/16
ChemScene
Product number
CS-0062825
Product name
AMG333
Purity
99.76%
Packaging
50mg
Price
$690
Updated
2021/12/16
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AMG-333 Chemical Properties,Usage,Production

Uses

AMG 333 is an orally active and highly selective TRPM8 antagonist with an IC50 of 13 nM.

in vivo

AMG 333 (0.6-3 mg/kg, p.o., single dose) dose-dependently inhibits wet-dog shake behavior in the Icilin (HY-11062)-induced wet-dog shake Sprague?Dawley rat model, demonstrating that AMG 333 effectively blocks the TRPM8 target[1]. AMG 333 (1-3 mg/kg, p.o., single dose) dose-dependently blocks blood pressure elevation in the cold stimulation-induced blood pressure elevation Sprague?Dawley rat model, indicating that AMG 333 effectively acts on the TRPM8 target[1].

Animal Model:Icilin (HY-11062)-induced wet-dog shake (WDS) behavior in Sprague?Dawley rat model[1]
Dosage:0.6, 1, 3 mg/kg
Administration:Oral gavage (p.o.), single dose
Result:Demonstrated significant dose-dependent inhibition; 3 mg/kg fully inhibited WDS.
Animal Model:Cold stimulation-induced blood pressure elevation Sprague?Dawley rat model[1]
Dosage:1, 3 mg/kg
Administration:Oral gavage (p.o.), single dose
Result:Showed significant inhibition of cold-induced blood pressure elevation at 1 mg/kg and 3 mg/kg; 3 mg/kg fully blocked cold-pressor response.

storage

Store at -20°C

References

[1] Horne DB, et al. Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine. J Med Chem. 2018 Sep 27;61(18):8186-8201. DOI:10.1021/acs.jmedchem.8b00518

AMG-333 Preparation Products And Raw materials

Raw materials

Preparation Products

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1416799-28-4, AMG-333Related Search:


  • AMG-333
  • AMG333;AMG 333
  • 3-Pyridinecarboxylic acid, 6-[[[(S)-(3-fluoro-2-pyridinyl)[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]amino]carbonyl]-
  • Inhibitor,AMG333,TRP Channel,inhibit,Transient receptor potential channels,AMG 333
  • (S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid
  • AMG 333, 10 mM in DMSO
  • AMG-333 ,S6638
  • 1416799-28-4
  • C20H12F5N3O4