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Chemical Structure| 328565-16-8 Chemical Structure| 328565-16-8

Structure of Col003
CAS No.: 328565-16-8

Chemical Structure| 328565-16-8

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Col003 is a cell penetrant, selective and potent inhibitor of the interaction of Hsp47 with collagen. Col003 is the cleavage product of AK778.It competitively inhibited the interaction and caused the inhibition of collagen secretion by destabilizing the collagen triple helix.

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Product Details of Col003

CAS No. :328565-16-8
Formula : C14H11NO4
M.W : 257.24
SMILES Code : O=CC1=CC(CC2=CC=CC=C2)=CC([N+]([O-])=O)=C1O
MDL No. :MFCD00852947
InChI Key :RKJXVCLOGNLZOI-UHFFFAOYSA-N
Pubchem ID :871077

Safety of Col003

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Col003

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human normal liver L02 cells 25, 50, 100 μM 24 h To assess the cytotoxicity of Col003 on L02 cells. Results showed that 25 and 50 μM Col003 had minimal impact on cell viability (>89.22%). Front Pharmacol. 2022 Jan 10;12:792263
Rat platelets 25 or 50 μM 5 min To evaluate the inhibitory effect of Col003 on collagen-induced platelet aggregation. Results showed that 50 μM Col003 significantly inhibited collagen-induced platelet aggregation. Front Pharmacol. 2022 Jan 10;12:792263
mouse embryonic fibroblasts (MEF) 100 μM 72 h Evaluate the inhibitory effect of Col003 on collagen secretion, results showed that Col003 significantly inhibited collagen secretion and accumulation J Biol Chem. 2017 Dec 8;292(49):20076-20085
LLC1-BMT5 cells 4.68 μM 24 h To evaluate the inhibitory effect of Col003 on COL1 secretion in LLC1-BMT5 cells, results showed that Col003 significantly reduced COL1 secretion Cell Rep Med. 2024 May 21;5(5):101533
4T1-BMT5 cells 3.96 μM 24 h To evaluate the inhibitory effect of Col003 on COL1 secretion in 4T1-BMT5 cells, results showed that Col003 significantly reduced COL1 secretion Cell Rep Med. 2024 May 21;5(5):101533
Adult mouse cardiac fibroblasts (AMCFs) 50 μM 48 h To evaluate the inhibitory effect of Col003 on hypoxia-reoxygenation (HR)-induced fibrogenesis. Results showed that Col003 inhibited HR-induced fibrogenesis, reduced the expression of collagen I and CTGF, and impeded the activation of the TGF-β1-Smad4 pathway. Acta Pharm Sin B. 2022 Nov;12(11):4138-4153

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J male mice DEN/CCl4-induced liver cancer model Intraperitoneal injection 10 mg/kg Twice weekly for 11 weeks Targeting SERPINH1 significantly delayed tumor occurrence and progression, reduced liver fibrosis and tumor burden Int J Biol Sci. 2024 Sep 23;20(13):5191-5207
Sprague-Dawley rats FeCl3-induced carotid artery thrombosis model and MCAO model Tail vein injection 25, 50, 100 μM Single dose To evaluate the protective effects of Col003 on thrombus formation and cerebral ischemia-reperfusion injury in vivo. Results showed that 50 μM Col003 significantly prolonged the time to thrombus formation and reduced cerebral infarct volume. Front Pharmacol. 2022 Jan 10;12:792263

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.89mL

0.78mL

0.39mL

19.44mL

3.89mL

1.94mL

38.87mL

7.77mL

3.89mL

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

References

 

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