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Migalastat hydrochloride (Synonyms: GR181413A)

Cat. No.: HY-14929A Purity: >98.0%
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 (GR181413A) hydrochloride 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.

In Vivo

Fabry 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 (GR181413A) 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 (GR181413A) hydrochloride reduces tissue GL-3 in fabry transgenic mice, and in urine and kidneys of some FD patients. Oral administration of Migalastat (GR181413A) 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].

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

Clinical Trial
Molecular Weight

199.63

Formula

C₆H₁₄ClNO₄

CAS No.

75172-81-5

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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.
References
Animal Administration
[2]

Mice: Migalastat (GR181413A) 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].

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

References
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Keywords:

MigalastatGR181413AOthersInhibitorinhibitorinhibit

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Migalastat hydrochloride
Cat. No.:
HY-14929A
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