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Mizagliflozin

Cat. No. M30450
Mizagliflozin Structure
Synonym:

DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base

Size Price Availability Quantity
5mg USD 198  USD198 In stock
10mg USD 340  USD340 In stock
25mg USD 680  USD680 In stock
50mg USD 980  USD980 In stock
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Quality Control & Documentation
Biological Activity

Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.

Chemical Information
Molecular Weight 564.67
Formula C28H44N4O8
CAS Number 666843-10-3
Form Solid
Solubility (25°C) Water ≥ 100 mg/mL (ultrasonic)
Storage 4°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nanae Ishida, et al. Pharmacol Res Perspect. Mizagliflozin, a selective SGLT1 inhibitor, improves vascular cognitive impairment in a mouse model of small vessel disease

[2] Pavit Luthra, et al. Lancet Gastroenterol Hepatol. Efficacy of drugs in chronic idiopathic constipation: a systematic review and network meta-analysis

[3] Shin Fukudo, et al. J Neurogastroenterol Motil. Effect of Mizagliflozin on Postprandial Plasma Glucose in Patients With Functional Constipation

[4] Christopher J Black, et al. Gastroenterology. Mizagliflozin for the Treatment of Functional Constipation: Are New Drugs Better?

[5] Toshihiro Inoue, et al. Eur J Pharmacol. Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation

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Keywords: Mizagliflozin, DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base supplier, SGLT, inhibitors, activators


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