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Cat. No.: HY-162459

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cGAS-IN-3

cGAS-IN-3 (compound 30d-S) is an orally active cyclic GMP-AMP synthase (Cyclic GMP-AMP Synthase/cGAS) inhibitor with good plasma exposure and low clearance. cGAS-IN-3 has anti-inflammatory activity and can significantly reduce lung inflammation in rats.

For research use only. We do not sell to patients.

Formula: C₂₁H₂₀Cl₂F₂N₄O₂
Molecular Weight:469.31

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (278 KB)

cGAS-IN-3 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

cGAS^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
THP1-Dual	CC₅₀	14.2 μM Compound: 30d-R	Cytotoxicity against human THP1-Dual cells incubated for 24 hrs by CCK-8 method Cytotoxicity against human THP1-Dual cells incubated for 24 hrs by CCK-8 method	[PMID: 38619191]

In Vitro

The inhibitory potency (IC₅₀) of cGAS-IN-3 against cGAS in mouse RAW-Lucia cells is 2.87 μM^[1].

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

In Vivo

cGAS-IN-3 (30 mg/kg; po; single dose) has preventive effects on LPS-induced acute lung injury (ALI) mouse model and can effectively reduce inflammation^[1].

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

Animal Model:

LPS-induced acute lung injury (ALI) mice model^[1]
Dosage:

30 mg/kg
Administration:

po; single dose and 0.5 h prior to ALI modeling; while ALI was induced by intratracheal instillation of 2 mg/kg LPS
Result:

Alleviated the severity of lung injury, presented by the ameliorated pathological changes
Relieved pulmonary edema, and the reduced number of immune cells in BALF.

Chemical Information

Molecular Weight 469.31
Formula C₂₁H₂₀Cl₂F₂N₄O₂
SMILES

ClC1=CC(C2=NN(C=C2)C(F)F)=C3C(NC4=C3C[C@]5(CC4)CCN(C5)C(CO)=O)=C1Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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)

References

[1]. Chen M, et al. Design, Synthesis, and Pharmacological Evaluation of Spiro[carbazole-3,3'-pyrrolidine] Derivatives as cGAS Inhibitors for Treatment of Acute Lung Injury. J Med Chem. 2024 Apr 25;67(8):6268-6291. [Content Brief]

Calculators

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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.

Keywords

100 mg

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