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Migalastat hydrochloride

CAS No. : 75172-81-5

MCE 站：Migalastat hydrochloride

产品活性：Migalastat hydrochloride (GR181413A) 是一种有效和竞争性的α-galactosidase A抑制剂，对人α-Gal A的 IC₅₀值为0.04 μM。

研究领域：Others

作用靶点：Others

In Vitro: Both IC₅₀ and K_i values of Migalastat (GR181413A) hydrochloride toward human lysosomal a-Gal A are 0.04 μM.

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. 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.

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