Art. -Nr.: HY-112340

CB1 antagonist 4

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CB1 antagonist 4 (compound 8) is a selective cannabinoid receptor 1 (CB1) inverse agonist with an IC₅₀ of 8.5 nM for human CB1. CB1 antagonist 4 shows selective for CB1 over CB2 receptors (IC₅₀ of 604.9 nM). CB1 antagonist 4 inhibits GTP binding to CB1-overexpressing cell membranes with an EC₅₀ of 18.5 nM.

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Reinheit: 98.00%
CAS. Nr.: 1253641-65-4
Formel: C₃₀H₂₅Cl₂F₃N₄OS
Molecular Weight:617.51

Speicherung:

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

CB1 antagonist 4 Chemical Structure

CAS. Nr.: 1253641-65-4

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CB1

8.5 nM (IC₅₀)

hCB2-R

604.9 nM (IC₅₀)

Alle Cannabinoid Receptor Isoform-spezifische Produkte anzeigen :

Chemical Information

CAS. Nr. 1253641-65-4
Appearance Solid
Molecular Weight 617.51
Formel C₃₀H₂₅Cl₂F₃N₄OS
Color Off-white to light yellow
SMILES

O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(C#CC4=CC=C(C(F)(F)F)C=C4)S3)=C1CC)NN5CCCCC5
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 : 41.67 mg/mL (67.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.6194 mL

8.0970 mL

16.1941 mL

5 mM

0.3239 mL

1.6194 mL

3.2388 mL

10 mM

0.1619 mL

0.8097 mL

1.6194 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 90% Corn Oil

Solubility: ≥ 4.17 mg/mL (6.75 mM); Clear solution

This protocol yields a clear solution of ≥ 4.17 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 (41.7 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 (272 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Hung MS, et al. Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist. ChemMedChem. 2010 Sep 3;5(9):1439-43. [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	1.6194 mL	8.0970 mL	16.1941 mL	40.4852 mL
	5 mM	0.3239 mL	1.6194 mL	3.2388 mL	8.0970 mL
	10 mM	0.1619 mL	0.8097 mL	1.6194 mL	4.0485 mL
	15 mM	0.1080 mL	0.5398 mL	1.0796 mL	2.6990 mL
	20 mM	0.0810 mL	0.4049 mL	0.8097 mL	2.0243 mL
	25 mM	0.0648 mL	0.3239 mL	0.6478 mL	1.6194 mL
	30 mM	0.0540 mL	0.2699 mL	0.5398 mL	1.3495 mL
	40 mM	0.0405 mL	0.2024 mL	0.4049 mL	1.0121 mL
	50 mM	0.0324 mL	0.1619 mL	0.3239 mL	0.8097 mL
	60 mM	0.0270 mL	0.1350 mL	0.2699 mL	0.6748 mL

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CB1 antagonist 4

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Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alkyne Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Alle Cannabinoid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CB1 antagonist 4

Anti-Obesity Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alkyne Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Alle Cannabinoid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CB1 antagonist 4 Related Classifications

HY-112340 Related Classifications