82186-71-8
Chemical Structure
Halofuginone lactate
Synonym(s): RU-19110 lactate
- CAS No.: 82186-71-8
- Formula:C19H23BrClN3O6
- Molecular Weight:504.76
IUPAC Name: 7-bromo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one 2-hydroxypropanoate
InChIKey: GATQERNJKZPJNX-LDXVYITESA-N
SMILES: OC(C(O)C)=O.O=C1C2=CC(Cl)=C(Br)C=C2N=CN1CC(C[C@H]3[C@@H](CCCN3)O)=O
Biological Activity: Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM[1][2]. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3][4]. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects[5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Halofuginone lactate | 98.32% | Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects. | ||||||||||||||||||||
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- [1]. Tsuchida K, et al. Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation. Free Radic Biol Med. 2017 Feb;103:236-247. [Content Brief]
- [2]. Keller TL, et al. Halofuginone and other Febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7. [Content Brief]
- [3]. Cui Z, et al. Halofuginone attenuates osteoarthritis by inhibition of TGF-β activity and H-type vessel formation in subchondral bone. Ann Rheum Dis. 2016 Sep;75(9):1714-21. [Content Brief]
- [4]. Tracy L McGaha, et al. Halofuginone, an inhibitor of type-I collagen synthesis and skin sclerosis, blocks transforming-growth-factor-beta-mediated Smad3 activation in fibroblasts. J Invest Dermatol. 2002 Mar;118(3):461-70. [Content Brief]
- [5]. Pritesh P Jain, et al. Halofuginone, a Promising Drug for Treatment of Pulmonary Hypertension. Br J Pharmacol. 2021 Mar 10. [Content Brief]
Keywords
