Halofuginone Hydrobromide


Catalog No. size PriceQuantity
M6885-2 2mg solid $128
M6885-10 10mg solid $533

Description

Cas:64924-67-0

Product Information

Halofuginone Hydrobromide is a potent prolyl-tRNA synthetase inhibitor.

 

Chemical Formula: C16H18Br2ClN3O3

 

Exact Mass: 492.9403

 

Molecular Weight: 495.6

 

Elemental Analysis: C, 38.78; H, 3.66; Br, 32.25; Cl, 7.15; N, 8.48; O, 9.68

Synonym:

 

Halofuginone HBr

 

Chemical Name: (2R*,3S*)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4-3H-quinazolinone hydrobromide

 

InChi Key: 

SJUWEPZBTXEUMU-LIOBNPLQSA-N

 

InChi Code: InChI=1S/C16H17BrClN3O3.BrH/c17-11-6-13-10(5-12(11)18)16(24)21(8-20-13)7-9(22)4-14-15(23)2-1-3-19-14;/h5-6,8,14-15,19,23H,1-4,7H2;1H/t14-,15+;/m1./s1

 

Smiles Code:

O=C1N(CC(C[C@H]2NCCC[C@@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3.[H]Br

 

 

Technical Data:

 

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

 

In Vitro:

Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase.

The IC50s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.

The IC50s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively.

 

In Vivo

Halofuginone (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage[.

Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone.

 

 

References

 

  1. Zhang J, Yao Q, Liu Z. A Novel Synthesis of the Efficient Anti-Coccidial Drug Halofuginone Hydrobromide. Molecules. 2017 Jun 30;22(7). pii: E1086. doi: 10.3390/molecules22071086. PubMed PMID: 28665346.

 

  1. Zhang DF, Sun BB, Yue YY, Yu HJ, Zhang HL, Zhou QJ, Du AF. Anticoccidial effect of halofuginone hydrobromide against Eimeria tenella with associated histology. Parasitol Res. 2012 Aug;111(2):695-701. doi: 10.1007/s00436-012-2889-7. Epub 2012 Mar 14. PubMed PMID: 22415441.

 

  1. Lista S, Emanuele E. Potential therapeutical effects of topical halofuginone hydrobromide in keloid management. Med Hypotheses. 2007;69(3):707. Epub 2007 Feb 28. PubMed PMID: 17331662.

 

  1. Holland DC, Munns RK, Roybal JE, Hurlbut JA, Long AR. Liquid chromatographic determination of the anticoccidial drug halofuginone hydrobromide in eggs. J AOAC Int. 1995 Jan-Feb;78(1):37-40. PubMed PMID: 7703725.

 

  1. Determination of halofuginone hydrobromide in medicated animal feeds. Analyst. 1983 Oct;108(1291):1252-6. PubMed PMID: 6650842.

 

Products are for research use only. Not for human use.

 

 

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