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
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
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.
N-Bromosuccinimide Price
- Product number
- 6874
- Product name
- AMG333
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $715
- Updated
- 2021/12/16
- Product number
- CS-0062825
- Product name
- AMG333
- Purity
- 99.76%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-0062825
- Product name
- AMG333
- Purity
- 99.76%
- Packaging
- 10mg
- Price
- $160
- Updated
- 2021/12/16
- Product number
- CS-0062825
- Product name
- AMG333
- Purity
- 99.76%
- Packaging
- 25mg
- Price
- $380
- Updated
- 2021/12/16
- Product number
- CS-0062825
- Product name
- AMG333
- Purity
- 99.76%
- Packaging
- 50mg
- Price
- $690
- Updated
- 2021/12/16
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
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