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Migalastat hydrochloride  (Synonyms: GR181413A)

Cat. No.: HY-14929A Purity: ≥98.0%
COA Handling Instructions

Migalastat hydrochloride (GR181413A) 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.

For research use only. We do not sell to patients.

Migalastat hydrochloride Chemical Structure

Migalastat hydrochloride Chemical Structure

CAS No. : 75172-81-5

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Based on 1 publication(s) in Google Scholar

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Description

Migalastat hydrochloride (GR181413A) 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.

IC50 & Target

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

Both IC50 and Ki values of Migalastat hydrochloride (GR181413A) toward human lysosomal a-Gal A are 0.04 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

Cell Line: EHK cells mutated α-Gal A
Concentration: 10 μM
Incubation Time: 9 days
Result: Reduced Gb3 accumulation and lysosome volume.
In Vivo

Fabry disease is an X-linked recessive disorder caused by the deficient activity of α-galactosidase A[2].
Migalastat (oral gavage, 3 mg/kg daily for 4 weeks) increases α-Gal A activity in heart, kidney, spleen, and liver in a dose- and time-dependently in transgenic mice that express human mutant alpha-Gal A (TgM)[2].
Migalastat shows the half-life of less than 1 day in all major issues in TgM for 2 weeks pretreatment[2].
Migalastat (oral gavage, 100 mg/kg daily for 28 days) to transgenic mice reduces lyso-Gb3 levels up to 64%, 59%, and 81% in kidney, heart, and skin, respectively[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male nontransgenic (Non-Tg) C57BL/6 mice; transgenic mice expressing human mutant R301Q α-Gal A (TgM), α-Gal A knockout mice (KO), mice express human R301Q α-Gal A in a null background (TgM/KO)[2]
Dosage: 3 mg/kg
Administration: Oral gavage; every day for 4 weeks
Result: Reduced Globotriaosylceramide (Gb3) storage remarkably in kidney of mice.
Clinical Trial
Molecular Weight

199.63

Appearance

Solid

Formula

C6H14ClNO4
CAS No.
SMILES
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

H2O : ≥ 200 mg/mL (1001.85 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.0093 mL 25.0463 mL 50.0927 mL
5 mM 1.0019 mL 5.0093 mL 10.0185 mL
10 mM 0.5009 mL 2.5046 mL 5.0093 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (500.93 mM); Clear solution; Need ultrasonic

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: ≥98.0%

COA (250 KB) HNMR (119 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Migalastat75172-81-5GR181413AOthersFabry diseaseorally activeα-galactosidase Aα-Gal AglobotriaosylceramideGb3globotriaosylsphingosinelyso-Gb1-deoxygalactonojirimycinDGJInhibitorinhibitorinhibit

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