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Targapremir-210

Cat. No. M27715
Targapremir-210 Structure
Synonym:

TGP-210

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Biological Activity

Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM).

Chemical Information
Molecular Weight 592.69
Formula C32H36N10O2
CAS Number 1049722-30-6
Form Solid
Solubility (25°C) DMSO 250 mg/mL (ultrasonic)
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] Matthew G Costales, et al. Cell Chem Biol. Targeted Degradation of a Hypoxia-Associated Non-coding RNA Enhances the Selectivity of a Small Molecule Interacting with RNA

[2] Matthew G Costales, et al. J Am Chem Soc. Small Molecule Inhibition of microRNA-210 Reprograms an Oncogenic Hypoxic Circuit

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Keywords: Targapremir-210, TGP-210 supplier, MicroRNA (miRNA), inhibitors, activators


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