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Halofuginone hydrobromide

Cat. No. M13648
Halofuginone hydrobromide Structure
Synonym:

RU-19110 hydrobromide

Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 140  USD140 In stock
25mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

Chemical Information
Molecular Weight 495.59
CAS Number 64924-67-0
Solubility (25°C) DMSO 50 mg/mL
Water 2.6 mg/mL
Storage 2-8°C, dry, 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] Pritesh P Jain, et al. Br J Pharmacol. Halofuginone, a promising drug for treatment of pulmonary hypertension

[2] Runan Zuo, et al. Int J Nanomedicine. Encapsulating Halofuginone Hydrobromide in TPGS Polymeric Micelles Enhances Efficacy Against Triple-Negative Breast Cancer Cells

[3] FEEDAP, et al. EFSA J. Safety and efficacy of STENOROL ® (halofuginone hydrobromide) as a feed additive for chickens for fattening and turkeys

[4] Zhuang Cui, et al. Ann Rheum Dis. Halofuginone attenuates osteoarthritis by inhibition of TGF-β activity and H-type vessel formation in subchondral bone

[5] Noel P McLaughlin, et al. Bioorg Med Chem. The chemistry and biology of febrifugine and halofuginone

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Keywords: Halofuginone hydrobromide, RU-19110 hydrobromide supplier, DNA/RNA Synthesis, inhibitors, activators


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