Glucosylceramide synthase-IN-2 - ≥98% , CAS No.2597958-02-4

CAS: 2597958-02-4 Cat. No.: G650816 Molecular Weight: 447.41

GRADE & PURITY ≥98%

Storage

Store at 2-8°C,Protected from light,Desiccated

Shipped In

Wet ice

Overview

Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC 50 s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research.

In Vitro

Glucosylceramide synthase-IN-2 (compound T-690) has no SERT inhibitory activity (IC 50 >10 μM). Glucosylceramide synthase-IN-2 does not affect GCase activity (EC 50 >300 μM). Glucosylceramide synthase-IN-2 (30 μM) does not potently inhibit hERG, Ca V 1.2, and Na V 1.5 channels. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Glucosylceramide synthase-IN-2 (compound T-690; po; 30, 100, 300 mg/kg) reduces GlcCer concentrations in the plasma and cerebral cortex in a dose-dependent manner in C57BL/6J mice . Glucosylceramide synthase-IN-2 (po; 5 mg/kg) has a C max of 416 ng/mL. Glucosylceramide synthase-IN-2 shows good oral exposure (BA = 31%) . Glucosylceramide synthase-IN-2 reveals good brain exposure (Cu,brain = 0.21 μM at 30 mg/kg dosing, 1 h) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC 50 s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits non

Storage

Store at 2-8°C, Protected from light, Desiccated

Shipped In

Wet ice

This product requires cold chain shipping. Ground and other economy services are not available.

Purity

≥98%

Names and Identifiers

• Canonical Smiles: O=C(C1=CC=NN(C1=O)C2=C(OCC(F)(F)F)C=CC=C2)NC3=CC=C(C(C)(O)C)C=C3
• Molecular Weight: 447.41

Chemical and Physical Properties

• Solubility: DMSO : 100 mg/mL (223.51 mM; Need ultrasonic)