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Chemical Structure| 99519-84-3 Chemical Structure| 99519-84-3

Structure of Carboxyamidotriazole
CAS No.: 99519-84-3

Chemical Structure| 99519-84-3

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Carboxyamidotriazole is a blocker of non-voltage dependent calcium channel with anti-inflammatory activity.

Synonyms: L-651582; CAI; RFE-007

4.5 *For Research Use Only !

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Product Details of Carboxyamidotriazole

CAS No. :99519-84-3
Formula : C17H12Cl3N5O2
M.W : 424.67
SMILES Code : O=C(C1=C(N)N(CC2=CC(Cl)=C(C(C3=CC=C(Cl)C=C3)=O)C(Cl)=C2)N=N1)N
Synonyms :
L-651582; CAI; RFE-007
MDL No. :MFCD00866325

Safety of Carboxyamidotriazole

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P264-P270-P301+P310+P330-P405-P501
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Description
Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways, which shows anti-tumor, anti-inflammatory and antiangiogenic effects[1].[2].

In Vitro:

Cell Line
Concentration Treated Time Description References
rat aortic rings 12 μg/mL 4 days as a positive control to evaluate anti-angiogenic properties Mol Cancer Ther. 2015 Oct;14(10):2228-37
HCT116 cells 10 μM 24 h CAI enhanced the cytotoxic activity of CD8+T cells against HCT116 cells. J Immunother Cancer. 2019 Sep 11;7(1):246
B16 melanoma cells 10 μM 24 h CAI enhanced the cytotoxic activity of CTLs against B16 melanoma cells and increased IFN-γ release. J Immunother Cancer. 2019 Sep 11;7(1):246
C26 cells 10 μM 48 h CAI inhibited complex I activity, increased ROS production, and enhanced glutamine metabolism and GSH levels. Acta Pharm Sin B. 2022 Feb;12(2):759-773
HCT116 cells 10 μM 48 h CAI inhibited glucose metabolism and fatty acid uptake, increased mitochondrial activity, but induced low levels of apoptosis. Acta Pharm Sin B. 2022 Feb;12(2):759-773

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/Ltj mice Sjögren's disease-like model Intragastric (i.g.) 20 and 40 mg/kg Once daily for 16 weeks To evaluate the therapeutic effect of CAI on Sj?gren's disease-like NOD/Ltj mice. Results showed that CAI significantly increased salivary secretion, reduced water intake, decreased serum autoantibody levels, suppressed histological alterations and lymphocyte infiltration, and reduced inflammatory factors such as IL-1β and IL-6. Int J Med Sci. 2025 Apr 28;22(10):2362-2372
Lewis rats Adjuvant arthritis (AA) model Oral 10, 20, 40 mg/kg Once daily from day 12 to day 26 To evaluate the therapeutic effects of CAI on AA rats, results showed that CAI dose-dependently decreased the arthritis index, improved radiological and histological changes, and reduced synovial levels of IL-1β, IL-6, IL-18 and TNF-α. Br J Pharmacol. 2015 Jul;172(13):3446-59
C57BL/6 mice B16 melanoma model Intragastric injection 20 mg/kg Once daily for 23 days CAI delayed the growth of B16 melanoma and increased IFN-γ levels in tumor tissues. J Immunother Cancer. 2019 Sep 11;7(1):246
BALB/c mice and nude mice Colorectal cancer xenograft model Intragastric injection 20 mg/kg CAI: once daily; CB-839: every 2 days; duration: 28 days CAI alone slightly inhibited tumor growth, while combination with GLS or GDH1 inhibitors significantly suppressed tumor growth and prolonged mouse survival. Acta Pharm Sin B. 2022 Feb;12(2):759-773

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.77mL

2.35mL

1.18mL

23.55mL

4.71mL

2.35mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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