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Col003 

Cat. No. M29916
Col003  Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 270  USD270 In stock
50mg USD 420  USD420 In stock
100mg USD 650  USD650 In stock
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Quality Control & Documentation
Biological Activity

Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis[1]

Chemical Information
Molecular Weight 257.24
Formula C14H11NO4
CAS Number 328565-16-8
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
Storage 4°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Saiyang Xie, et al. Acta Pharm Sin B. Cardiac fibroblast heat shock protein 47 aggravates cardiac fibrosis post myocardial ischemia-reperfusion injury by encouraging ubiquitin specific peptidase 10 dependent Smad4 deubiquitination

[2] Shuang Wu, et al. Front Pharmacol. Hsp47 Inhibitor Col003 Attenuates Collagen-Induced Platelet Activation and Cerebral Ischemic-Reperfusion Injury in Rats

[3] Masahito Yoshida, et al. Chem Pharm Bull (Tokyo). Structure-Activity Relationship Study on Col-003, a Protein-Protein Interaction Inhibitor between Collagen and Hsp47

[4] Shinya Ito, et al. J Biol Chem. A BRET-based assay reveals collagen-Hsp47 interaction dynamics in the endoplasmic reticulum and small-molecule inhibition of this interaction

[5] Shinya Ito, et al. J Biol Chem. A small-molecule compound inhibits a collagen-specific molecular chaperone and could represent a potential remedy for fibrosis

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  Catalog
Abmole Inhibitor Catalog




Keywords: Col003  supplier, HSP, inhibitors, activators


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