Art. -Nr.: HY-112703

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AMG 333

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

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Reinheit: 99.82%
CAS. Nr.: 1416799-28-4
Formel: C₂₀H₁₂F₅N₃O₄
Molecular Weight:453.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AMG 333 Chemical Structure

CAS. Nr.: 1416799-28-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

IC50: 13 nM (TRPM8)^[1]

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1416799-28-4
Appearance Solid
Molecular Weight 453.32
Formel C₂₀H₁₂F₅N₃O₄
Color White to off-white
SMILES

FC1=CC=CN=C1[C@H](C2=CC(F)=C(OC(F)(F)F)C=C2)NC(C3=NC=C(C(O)=O)C=C3)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 125 mg/mL (275.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2059 mL

11.0297 mL

22.0595 mL

5 mM

0.4412 mL

2.2059 mL

4.4119 mL

10 mM

0.2206 mL

1.1030 mL

2.2059 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.17 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.17 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.17 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2059 mL	11.0297 mL	22.0595 mL	55.1487 mL
	5 mM	0.4412 mL	2.2059 mL	4.4119 mL	11.0297 mL
	10 mM	0.2206 mL	1.1030 mL	2.2059 mL	5.5149 mL
	15 mM	0.1471 mL	0.7353 mL	1.4706 mL	3.6766 mL
	20 mM	0.1103 mL	0.5515 mL	1.1030 mL	2.7574 mL
	25 mM	0.0882 mL	0.4412 mL	0.8824 mL	2.2059 mL
	30 mM	0.0735 mL	0.3677 mL	0.7353 mL	1.8383 mL
	40 mM	0.0551 mL	0.2757 mL	0.5515 mL	1.3787 mL
	50 mM	0.0441 mL	0.2206 mL	0.4412 mL	1.1030 mL
	60 mM	0.0368 mL	0.1838 mL	0.3677 mL	0.9191 mL
	80 mM	0.0276 mL	0.1379 mL	0.2757 mL	0.6894 mL
	100 mM	0.0221 mL	0.1103 mL	0.2206 mL	0.5515 mL

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AMG 333

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG 333

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG 333 Related Classifications

HY-112703 Related Classifications