Art. -Nr.: HY-170362

cGAS-IN-4

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cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC₅₀ of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC₅₀ of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models. orally active, THP-1, C57Bl/6 mouse, orally active

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Reinheit: 99.28%
CAS. Nr.: 2987886-49-5
Formel: C₁₉H₁₈Cl₂N₄O₃
Molecular Weight:421.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

cGAS-IN-4 Chemical Structure

CAS. Nr.: 2987886-49-5

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

Biologische Aktivität

Beschreibung

cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC₅₀ of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC₅₀ of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models^[1]. orally active, THP-1, C57Bl/6 mouse, orally active

Chemical Information

CAS. Nr. 2987886-49-5
Appearance Solid
Molecular Weight 421.28
Formel C₁₉H₁₈Cl₂N₄O₃
Color White to off-white
SMILES

C[C@H]1C(C2=CC=C3Cl)=C(CCN1C(C4=NC=C(OCCO)C=N4)=O)NC2=C3Cl
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (237.37 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

2.3737 mL

11.8686 mL

23.7372 mL

5 mM

0.4747 mL

2.3737 mL

4.7474 mL

10 mM

0.2374 mL

1.1869 mL

2.3737 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 2.5 mg/mL (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (270 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Cyr P, et al., Discovery of Potent and Orally Bioavailable Pyrimidine Amide cGAS Inhibitors via Structure-Guided Hybridization. ACS Med Chem Lett. 2024 Nov 25;15(12):2201-2209. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3737 mL	11.8686 mL	23.7372 mL	59.3430 mL
	5 mM	0.4747 mL	2.3737 mL	4.7474 mL	11.8686 mL
	10 mM	0.2374 mL	1.1869 mL	2.3737 mL	5.9343 mL
	15 mM	0.1582 mL	0.7912 mL	1.5825 mL	3.9562 mL
	20 mM	0.1187 mL	0.5934 mL	1.1869 mL	2.9671 mL
	25 mM	0.0949 mL	0.4747 mL	0.9495 mL	2.3737 mL
	30 mM	0.0791 mL	0.3956 mL	0.7912 mL	1.9781 mL
	40 mM	0.0593 mL	0.2967 mL	0.5934 mL	1.4836 mL
	50 mM	0.0475 mL	0.2374 mL	0.4747 mL	1.1869 mL
	60 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9890 mL
	80 mM	0.0297 mL	0.1484 mL	0.2967 mL	0.7418 mL
	100 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5934 mL

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cGAS-IN-4

Immunology/Inflammation Compound Library

Orally Active Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Pattern Recognition Receptors Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

cGAS-IN-4

Immunology/Inflammation Compound Library

Orally Active Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Pattern Recognition Receptors Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

cGAS-IN-4 Related Classifications

HY-170362 Related Classifications