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Migalastat hydrochloride

Catalog No. T12038   CAS 75172-81-5
Synonyms: GR181413A hydrochloride, Migalastat HCl, GR181413A HCl

Migalastat hydrochloride (GR181413A) is an orally available, potent and competitive inhibitor of alpha-galactosidase A. It promotes the transport of alpha-galactosidase A to the lysosome and can be used in the study of Fabry disease.

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Migalastat hydrochloride Chemical Structure
Migalastat hydrochloride, CAS 75172-81-5
Pack Size Availability Price/USD Quantity
2 mg In stock $ 44.00
5 mg In stock $ 81.00
10 mg In stock $ 161.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Migalastat hydrochloride (GR181413A) is an orally available, potent and competitive inhibitor of alpha-galactosidase A. It promotes the transport of alpha-galactosidase A to the lysosome and can be used in the study of Fabry disease.
Targets&IC50 α-GalA (human):0.04 μM (Ki), α-GalA (human):0.04 μM
In vitro Migalastat hydrochloride (GR181413A) demonstrates IC50 and Ki values of 0.04 μM for human lysosomal alpha-Gal A[4].
In vivo Fabry disease is an X-linked recessive disorder caused by deficient activity of alpha-galactosidase A (α-Gal A)[2]. In transgenic mice expressing the mutant human α-Gal A (TgM), oral administration of Migalastat hydrochloride (3 mg/kg per day for 4 consecutive weeks) results in a dose- and time-dependent increase in α-Gal A activity in the heart, kidneys, spleen, and liver[2].After a 2-week pretreatment with Migalastat hydrochloride, the half-life for all major issues is less than 1 day[2]. Administration of Migalastat hydrochloride (100 mg/kg per day orally for 28 days) in transgenic mice leads to a reduction of 64%, 59%, and 81% in globotriaosylceramide (Gb3) levels in the kidneys, heart, and skin, respectively[3].
Synonyms GR181413A hydrochloride, Migalastat HCl, GR181413A HCl
Molecular Weight 199.63
Formula C6H14ClNO4
CAS No. 75172-81-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (250.46 mM)

TargetMolReferences and Literature

1. Welford RWD, et al. Glucosylceramide synthase inhibition with lucerastat lowers globotriaosylceramide and lysosome staining in cultured fibroblasts from Fabry patients with different mutation types. Hum Mol Genet. 2018 Oct. 27(19):3392-3403. 2. Ishii S, et al. Preclinical efficacy and safety of 1-deoxygalactonojirimycin in mice for Fabry disease. J Pharmacol Exp Ther. 2009 Mar;328(3):723-31. 3. Young-Gqamana B, et al. Migalastat HCl reduces globotriaosylsphingosine (lyso-Gb3) in Fabry transgenic mice and in the plasma of Fabry patients. PLoS One. 2013;8(3):e57631. 4. Asano N, et al. In vitro inhibition and intracellular enhancement of lysosomal alpha-galactosidase A activity in Fabry lymphoblasts by 1-deoxygalactonojirimycin and its derivatives. Eur J Biochem. 2000 Jul;267(13):4179-86.

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Keywords

Migalastat hydrochloride 75172-81-5 Others GR181413A hydrochloride Migalastat HCl GR181413A HCl GR181413A inhibitor inhibit

 

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