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CTS-1027

Cat. No. M14469
CTS-1027 Structure
Synonym:

Ro 1130830; RS 130830

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Biological Activity

CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.

Chemical Information
Molecular Weight 425.88
CAS Number 193022-04-7
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Fabian D Liechti, et al. The matrix metalloproteinase inhibitor RS-130830 attenuates brain injury in experimental pneumococcal meningitis

[2] A Tomillero, et al. Gateways to clinical trials

[3] Alisan Kahraman, et al. Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse

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  Catalog
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Keywords: CTS-1027, Ro 1130830; RS 130830 supplier, MMP, inhibitors, activators


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