1. Membrane Transporter/Ion Channel
  2. SGLT
  3. Tofogliflozin hydrate

Tofogliflozin hydrate (Synonyms: CSG-452 hydrate)

Cat. No.: HY-13413 Purity: 99.41%
Handling Instructions

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.

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

Tofogliflozin hydrate Chemical Structure

Tofogliflozin hydrate Chemical Structure

CAS No. : 1201913-82-7

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10 mM * 1 mL in DMSO USD 110 In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of Tofogliflozin hydrate:

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Description

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2. IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1] Target: SGLT2 inhibitor in vitro: Tofogliflozin competitively inhibited SGLT2 in cells overexpressing SGLT2, and K(i) values for human, rat, and mouse SGLT2 inhibition were 2.9, 14.9, and 6.4 nM, respectively. The selectivity of tofogliflozin toward human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 was the highest among the tested SGLT2 inhibitors under clinical development [1]. tofogliflozin was catalyzed to the primary hydroxylated derivative (M4) by CYP2C18, CYP4A11 and CYP4F3B, then M4 was oxidized to M1. 3. Tofogliflozin had no induction potential on CYP1A2 and CYP3A4 [4]. in vivo: A single oral gavage of tofogliflozin increased renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats. Tofogliflozin also improved postprandial glucose excursion in a meal tolerance test with GK rats. In db/db mice, 4-week tofogliflozin treatment reduced glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test 4 days after the final administration [1]. Tofogliflozin (400 ng/ml) induced UGE of about 2 mg/kg per min and increased EGP by 1-2 mg/kg per min, resulting in PG in the normal range [2]. Tofogliflozin suppressed plasma glucose and glycated Hb and preserved pancreatic beta-cell mass and plasma insulin levels. No improvement of glycaemic conditions or insulin level was observed with losartan treatment [3].

Clinical Trial
Molecular Weight

404.45

Formula

C₂₂H₂₈O₇

CAS No.

1201913-82-7

SMILES

O[[email protected]@H]1[[email protected]@H](O)[[email protected]](O)[[email protected]@H](CO)O[[email protected]@]21OCC3=C2C=C(CC4=CC=C(CC)C=C4)C=C3.O

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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: 

DMSO : ≥ 100 mg/mL (247.25 mM)

H2O : 0.33 mg/mL (0.82 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4725 mL 12.3625 mL 24.7249 mL
5 mM 0.4945 mL 2.4725 mL 4.9450 mL
10 mM 0.2472 mL 1.2362 mL 2.4725 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.41%

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Tofogliflozin hydrate
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