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Halofuginone hydrobromide, also known as HF, is a compound with the chemical formula C16H17BrClN3O3.HBr, CAS 64924-67-, The molecular weight is 495.59. Its molecular structure consists of a core skeleton of quinazolinone and substituents of bromine and chlorine atoms, including a pyridine ring and an acetone side chain, forming a unique stereoconformation.
This substance is a white to off white powder that is insoluble in water, methanol, and dimethyl sulfoxide, but can dissolve up to a concentration of 100 mM in dimethyl sulfoxide (DMSO). The storage conditions should be strictly controlled between -20 ℃ and 8 ℃ to avoid decomposition failure. As a low toxicity derivative of febrifugine extracted from Dichroa febrifuga, its pharmacokinetic properties have been optimized through chemical modification, making it a multi-target bioactive molecule.
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Halofuginone hydrobromide, as a compound extracted from traditional Chinese medicine Changshan and structurally modified, has shown wide application value in animal health, human disease treatment, and industrial fields due to its unique chemical properties and biological activity.
Animal health field: dual effects of anti parasitic and growth promoting
1. Core drugs for anti coccidiosis
It is a key drug for the prevention and control of coccidiosis in poultry farming, with strong inhibitory effects on the spores and fission bodies of six species of Eimeria, including Eimeria tenella and Eimeria toxigenic, with a minimum inhibitory concentration (MIC) of 0.1-0.5 μ g/mL. Its unique advantages lie in:
Blocking the transmission chain: completely inhibiting the expulsion of egg sacs after medication (except for Eimeria jirovecii), reducing the risk of environmental re pollution.
No cross resistance: Unlike existing anticoccidial drugs such as monensin and salinomycin, which have different mechanisms of action, they can be rotated to delay the development of resistance.
Promoting growth: Adding 2.72-5.44 g/ton (0.0003% -0.0006%) to feed can increase chicken weight gain by 5% -10% and feed conversion efficiency by 8% -12%.
Clinical application cases:
EU approval: In 2024, the European Commission issued Regulation (EU) 2024/231 approving halofotaxine hydrobromide as a feed additive for broiler chickens, turkeys, and breeding turkeys, under the authorized category of "anti coccidiosis agents and tissue trichomonas inhibitors", valid until 2034.
Chinese standard: The Ministry of Agriculture stipulates that the addition amount in chicken feed is 3 mg/kg, with a 4-day rest period to ensure the safety of animal food.
2. Adjuvant treatment for Taylor's disease
In ruminant animals such as cattle and sheep, other drugs (such as methylenebacterium salicylate peptide) can be combined to treat Tayloriosis by inhibiting the parasite's nucleic acid synthesis and blocking its proliferation. Research has shown that combination therapy can reduce animal mortality by 30% and increase cure rates to over 85%.
3. Synergistic strategies for combination therapy
Often used in combination with the following drugs to expand the antibacterial spectrum:
Methylsalicylic acid bacitracin: enhances the inhibitory effect on Gram positive bacteria and is used to prevent necrotizing enteritis in chickens.
Rosha swelling: synergistically anti coccidiosis, reducing single drug dosage, and lowering toxicity risk.
Bacitracin Zinc: Promotes intestinal microbiota balance and improves feed utilization efficiency.
Usage restrictions:
Prohibited for use in laying hens and waterfowl (such as ducks and geese) to prevent drug residues from being transmitted through the food chain.
Toxic to fish and aquatic organisms, should be used away from water sources.
Exploration in the field of human medicine: from anti-inflammatory to anti-tumor
1. Potential therapeutic drugs for osteoarthritis (OA)
Delaying the progression of OA through a dual mechanism:
Inhibition of TGF - β signaling pathway: reduces the formation of H-shaped blood vessels in subchondral bone, lowers bone remodeling activity, and thus protects articular cartilage.
Blocking prolyl tRNA synthetase: inhibits type I collagen synthesis and reduces cartilage fibrosis.
Animal experiments have shown that intraperitoneal injection at doses of 0.2-0.5 mg/kg can significantly reduce the cartilage injury score (OARSI score decreased by 40%) in mouse OA models.
Preclinical studies:
In the anterior cruciate ligament transection (ACLT) mouse model, treatment with halofodone hydrobromide (0.5 mg/kg) for one month resulted in a 25% increase in articular cartilage thickness and a 70% recovery of proteoglycan content to normal levels.
2. Innovative targets for tumor adjuvant therapy
Inhibiting tumor growth by regulating the NRF2 pathway:
Downregulation of NRF2 protein expression: In esophageal cancer (KYSE70) and lung cancer (A549) cells, IC ₅₀ were 114.6 nM and 58.9 nM, respectively, reducing NRF2 accumulation by promoting proteasomal degradation.
Enhanced chemotherapy sensitivity: Combined with cisplatin, it can synergistically inhibit tumor volume, with a tumor inhibition rate of 65% in the combination therapy group (30% -40% in the monotherapy group).
Mechanism of action:
Competitive binding to the proline binding pocket of proline tRNA synthase blocks proline incorporation into protein synthesis, leading to global protein synthesis inhibition (IC ₅₀: 22.6-45.7 nM) and inducing tumor cell apoptosis.
3. Intervention strategies for fibrotic diseases
In diseases such as systemic sclerosis and pulmonary fibrosis, collagen deposition is reduced by inhibiting TGF - β - induced fibroblast activation. In vitro experiments have shown that a concentration of 100 nM can reduce the secretion of type I collagen in fibroblasts by 60%, providing a new approach for the treatment of fibrotic diseases.
Industrial sector: diverse applications as chemical raw materials
1. Key intermediates in organic synthesis
The core structure of its quinazolinone makes halofuginone hydrobromide a precursor for synthesizing various bioactive molecules:
Drug synthesis: used for the preparation of antimalarial drugs, anti-tumor drugs, and derivatives of antibacterial drugs.
Materials Science: As a monomer for functionalized polymers, it is used to prepare photoluminescent materials or sensors.
2. Standard substances in analytical chemistry
Due to its stable chemical properties, it is used as:
Calibration standard for high-performance liquid chromatography (HPLC): used for quantitative analysis of compounds with similar structures.
Reference material for mass spectrometry (MS): Mass spectrometry fragments used to assist in the identification of quinazolinone compounds.
The discovery of Halofuginone Hydrobromamide is an important breakthrough in the fields of natural product chemistry and drug development. Its origin can be traced back to the traditional Chinese medicine Dichroa febrifuga, and its modern application embodies scientists' deep exploration of structural modification and mechanism of action.
The history of Changshan as a traditional Chinese medicine can be traced back to the Eastern Han Dynasty's "Shennong Bencao Jing", and its roots and stems were used to treat malaria. In the mid-20th century, scientists isolated the active ingredient Febrifugene from Changshan and found that it had potent anti malarial effects. However, the toxicity of Febrifugene, such as severe vomiting and liver damage, limits its clinical application. This contradiction has prompted researchers to turn to structural modification, attempting to reduce toxicity while retaining activity.
In the 1960s, the American company Cyanamid (later merged into the German company Hoechst Roussel Agri Vet) successfully synthesized halofuginone using febrifugine as a template by introducing bromine and chlorine atoms and optimizing the pyridine ring structure. This modification significantly reduces toxicity:
Toxicity data: The oral dose of LD ₅₀ in rats was 25 mg/kg, and in pregnant rats it was 33 mg/kg. Continuous administration for 30 days did not cause embryonic abnormalities, while the toxicity of Febrifune was several times higher.
Improvement in palatability: Although there is still a problem of poor palatability (a 15% -20% decrease in animal feed intake), it has the conditions for large-scale application.
In 1991, haloketone hydrobromide (trade name Stenolol) was approved by the US FDA, becoming the first chemically synthesized anti coccidiosis drug for avian coccidiosis, marking a crucial step in its transition from the laboratory to the market.
The unique value of haloketones lies in their multi-target mechanism of action:
Anti coccidiosis activity:
Inhibit the nucleic acid synthesis of microsporidia and schizonts, and block the proliferation cycle.
The MIC for 6 species of Eimeria, including Eimeria tenella and Eimeria toxin, is 0.1-0.5 μ g/mL, and there is no cross resistance with existing anti coccidial drugs.
Anti inflammation and anti fibrosis:
As an ATP competitive inhibitor of Prolyl tRNA Synthetase (Ki=18.3 nM), it blocks proline incorporation into protein synthesis and inhibits type I collagen production.
By inhibiting the TGF - β signaling pathway, reducing the formation of H-shaped blood vessels in subchondral bone, and delaying the progression of osteoarthritis (OA). Animal experiments have shown that doses of 0.2-0.5 mg/kg can significantly reduce cartilage injury scores in mouse OA models.
Antitumor potential:
In vitro experiments showed that its IC ₅₀ against esophageal cancer (KYSE70) and lung cancer (A549) cells were 114.6 nM and 58.9 nM, respectively, inducing tumor cell apoptosis by downregulating NRF2 protein expression.
Combined with cisplatin, halofuginone hydrobromide can synergistically inhibit tumor growth and increase tumor volume reduction rate by 40% compared to monotherapy.
Frequently Asked Questions
What is the brand name for halofuginone?
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Halofuginone, sold under the brand name Halocur, is a coccidiostat used in veterinary medicine. It is a synthetic halogenated derivative of febrifugine, a natural quinazolinone alkaloid which can be found in the Chinese herb Dichroa febrifuga (Chang Shan).
Is halofuginone used in human medicine?
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Halofuginone (HF), a derivative of febrifugine from antimalarial Chinese herbal medicine Changshan, is a Food and Drug Administration–approved, orally bioavailable drug used to treat scleroderma and protozoal infections.
Is halofuginone FDA approved?
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FDA Approval Status: Investigational. As of March 2026, halofuginone hydrobromide is not FDA-approved for human cancer treatment. It has previously received Orphan Drug Designation for conditions like Duchenne Muscular Dystrophy (DMD) and scleroderma.
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