1152425-66-5
1152425-66-5 structure
- Name: Luseogliflozin hydrate
- Chemical Name: (1S)-1,5-Anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol hydrate (1:1)
- CAS Number: 1152425-66-5
- Molecular Formula: C23H32O7S
- Molecular Weight: 452.56
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel SGLT
- Create Date: 2018-07-02 09:36:21
- Modify Date: 2024-01-02 16:42:31
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Luseogliflozin (TS 071) hydrate is a selective potent and orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor with an IC50 of 2.26 nM. Luseogliflozin hydrate can be used for the research of type 2 diabetes mellitus (T2DM)[1][2].
| Name | (1S)-1,5-Anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol hydrate (1:1) |
|---|---|
| Synonyms |
D-Glucitol, 1,5-anhydro-1-C-[5-[(4-ethoxyphenyl)methyl]-2-methoxy-4-methylphenyl]-1-thio-, (1S)-, hydrate (1:1)
(1S)-1,5-Anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol hydrate (1:1) |
| Description | Luseogliflozin (TS 071) hydrate is a selective potent and orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor with an IC50 of 2.26 nM. Luseogliflozin hydrate can be used for the research of type 2 diabetes mellitus (T2DM)[1][2]. |
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| Related Catalog | |
| Target |
IC50: 2.26 nM (SGLT2)[1][2] |
| In Vitro | Luseogliflozin can increase beta cell proliferation through the activation of the FoxM1/PLK1/CENP-A pathway via humoral factors thats act in an insulin/IGF-1 receptor-independent manner. Luseogliflozin increases beta cell proliferation in OSI-906-treated mice[2]. Cell Viability Assay[2] Cell Line: βIRKO, IRS1KO and IRS2KO beta cells Concentration: 100 nM Incubation Time: 24 and 48 hours Result: Cell Viability Assay[2]Treating cells with serum from the OSI-906 (200 nM) or OSI-906+Luseogliflozin(100 nM) group led to significantly increased cell viability in the latter group in the control, IRS1KO, IRS2KO, as well as the insulin receptor (IR)-deficient βIRKO beta cells. |
| In Vivo | SGLT2 inhibition with Luseogliflozin (10 mg/kg/daily; oral gavage) significantly ameliorates hyperglycaemia, but not hyperinsulinaemia, in the OSI-906(45 mg/kg)-treated mice. Luseogliflozin ameliorates hyperglycaemia induced by OSI-906[2]. Animal Model: C57BL/6J male mice aged 8 weeks old[2] Dosage: 10 mg/kg/daily Administration: Oral gavage; for 7 days between 08:00 and 09:00 hours Result: Treatment significantly ameliorated the OSI-906 (45 mg/kg)-induced hyperglycaemia. |
| References |
[1]. Anthony Markham,et al. Luseogliflozin: first global approval. Drugs. 2014 Jun;74(8):945-50. |
| Molecular Formula | C23H32O7S |
|---|---|
| Molecular Weight | 452.56 |
| Exact Mass | 452.186859 |