CAS 75172-81-5|Migalastat hydrochloride

Introduction:Basic information about CAS 75172-81-5|Migalastat hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameMigalastat hydrochloride
CAS Number75172-81-5Molecular Weight199.63300
Density/Boiling Point382.7ºC at 760 mmHg
Molecular FormulaC6H14ClNO4Melting Point260ºC
MSDSUSAFlash Point185.2ºC

Names

Namedeoxygalactonojirimycin, hydrochloride
SynonymMore Synonyms

Migalastat hydrochloride BiologicalActivity

DescriptionMigalastat hydrochloride (1-Deoxygalactonojirimycin hydrochloride) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
Related CatalogSignaling Pathways >>Others >>OthersResearch Areas >>Others
Target

IC50: 0.04 μM (human α-Gal A)[1];Ki: 0.04 μM (human α-Gal A)[1]

In VitroBoth IC50 and Ki values of migalastat hydrochloride toward human lysosomal a-Gal A are 0.04 μM[1].
In VivoFabry disease is an X-linked recessive disorder caused by the deficient activity of α-galactosidase A. α-Gal A activity in heart, kidney, spleen, and liver is increased dose- and time-dependently in transgenic mice that express human mutant alpha-Gal A with migalastat hydrochloride treatment. The half-life of DGJ is less than 1 day in all major issues and that of the enzyme synthesized during the DGJ treatment period is approximately 4 days[2]. Oral administration of migalastat hydrochloride reduces tissue GL-3 in fabry transgenic mice, and in urine and kidneys of some FD patients. Oral administration of migalastat hydrochloride to transgenic mice reduces elevated lyso-Gb3 levels up to 64%, 59%, and 81% in kidney, heart, and skin, respectively, generally equal to or greater than observed for GL-3[3].
Animal AdminMice: Migalastat hydrochloride is dissolved in drinking water. Age-matched male homozygous TgM, TgM/KO, and nontransgenic (Non-Tg) C57BL/6 mice are supplied drinking water containing DGJ ad libitum. Body weight is monitored weekly during the DGJ treatment period. Average daily DGJ dosage is estimated based on the consumption of drinking water. Mice fed drinking water containing DGJ at 0.05 mM typically received DGJ at approximately 3 mg/kg body weight/day[2].
References

[1]. 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.

[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.

Chemical & Physical Properties

Boiling Point382.7ºC at 760 mmHg
Melting Point260ºC
Molecular FormulaC6H14ClNO4
Molecular Weight199.63300
Flash Point185.2ºC
Exact Mass199.06100
PSA92.95000
InChIKeyZJIHMALTJRDNQI-OLALXQGDSA-N
SMILESCl.OCC1NCC(O)C(O)C1O

Safety Information

Personal Protective Equipmentdust mask type N95 (US);Eyeshields;Gloves
Hazard CodesXi
Risk PhrasesR36/37/38
Safety Phrases26-36
RIDADRNONH for all modes of transport

Articles1

More Articles
Paulsen, H., et al.

Chem. Ber. 113 , 2601, (1980)

Synonyms

(1R,3R,4R,5S)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidinium chloride
1,5-dideoxy-1,5-imino-D-glucitol hydrochloride
1-Deoxymannojirimycinehydrochloride
DEOXYMANNONOJIRIMYCIN HCL
(+)-(2R,3R,4R,5S)-2-hydroxymethyl-3,4,5-trihydroxypiperidine hydrochloride
DEOXYMANNOJIRIMYCIN,HYDROCHLORIDE
(+)-1-deoxynojirimycin hydrochloride
1-DEOXYMANNOJIRIMYCIN HCL
DMM
DEOXYMANNOJIRIMYCIN HCL
DMJ,HYDROCHLORIDE
1-DeoxymannojirimycineHCl
Migalastat (hydrochloride)
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