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MedKoo Cat#: 319583 | Name: Mizagliflozin
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Mizagliflozin, also known as DSP-3235, KGA-3235, GSK-1614235, is a sodium-glucose transporter inhibitor. It is expected to improve postprandial hyperglycemia by suppressing glucose absorption from the intestine with a novel mechanism of action different from that of conventional alpha-glucosidase inhibitors. Mizagliflozin blocks intestinal glucose absorption and reduce GIP secretion in rats and humans, suggesting SGLT1 glucose transport is critical for GIP release.

Chemical Structure

Mizagliflozin
Mizagliflozin
CAS#666843-10-3

Theoretical Analysis

MedKoo Cat#: 319583

Name: Mizagliflozin

CAS#: 666843-10-3

Chemical Formula: C28H44N4O8

Exact Mass: 564.3159

Molecular Weight: 564.68

Elemental Analysis: C, 59.56; H, 7.85; N, 9.92; O, 22.67

Price and Availability

Size Price Availability Quantity
25mg USD 850.00 2 Weeks
50mg USD 1,450.00 2 Weeks
100mg USD 1,950.00 2 Weeks
200mg USD 3,250.00 2 Weeks
500mg USD 4,650.00 2 Weeks
1g USD 5,950.00 2 Weeks
2g USD 8,950.00 2 Weeks
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Related CAS #
No Data
Synonym
DSP-3235, DSP3235; DSP 3235; KGA-3235; KGA 3235; KGA3235; GSK-1614235; GSK 1614235; GSK1614235; Mizagliflozin
IUPAC/Chemical Name
3-((3-(4-((5-isopropyl-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-1H-pyrazol-4-yl)methyl)-3-methylphenoxy)propyl)amino)-2,2-dimethylpropanamide
InChi Key
LREHMKLEOJAVMQ-TXKDOCKMSA-N
InChi Code
InChI=1S/C28H44N4O8/c1-15(2)21-19(25(32-31-21)40-26-24(36)23(35)22(34)20(13-33)39-26)12-17-7-8-18(11-16(17)3)38-10-6-9-30-14-28(4,5)27(29)37/h7-8,11,15,20,22-24,26,30,33-36H,6,9-10,12-14H2,1-5H3,(H2,29,37)(H,31,32)/t20-,22-,23+,24-,26+/m1/s1
SMILES Code
O=C(N)C(C)(C)CNCCCOC1=CC=C(CC2=C(C(C)C)NN=C2O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)C(C)=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1.
In vitro activity:
Both Pre‐ and Post‐treatment with mizagliflozin and phlorizin prevented cell death in IL‐1β‐treated PC12HS cells (Figure 8A). The Cell Counting Kit‐8 assay demonstrated that IL‐1β decreased the survival rate of PC12HS cells. Both mizagliflozin and phlorizin ameliorated IL‐1β‐induced decreases in the survival rate of PC12HS cells regardless of the administration start time (Figure 8B and B). Reference: Pharmacol Res Perspect. 2021 Oct;9(5):e00869. https://pubmed.ncbi.nlm.nih.gov/34586752/
In vivo activity:
The wire hang test showed that the latency to fall was shorter in saline‐treated ACAS (asymmetric common carotid artery surgery) compared with sham‐operated mice (Figure 3A). Moreover, ACAS significantly shortened the latency to fall in saline‐treated ACAS mice compared with mizagliflozin‐treated or phlorizin‐treated ACAS mice. (Figure 3A). Interestingly, the latency to fall was similar among sham‐operated mice, low or high concentrations of mizagliflozin‐treated ACAS mice, and phlorizin‐treated ACAS mice, indicating that mizagliflozin and phlorizin can improve the shortened latency to fall to the normal level in ACAS mice (Figure 3A). Reference: Pharmacol Res Perspect. 2021 Oct;9(5):e00869. https://pubmed.ncbi.nlm.nih.gov/34586752/
Solvent mg/mL mM comments
Solubility
DMSO 100.0 177.09
Ethanol 100.0 177.09
Water 100.0 177.09
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 564.68 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Ishida N, Saito M, Sato S, Tezuka Y, Sanbe A, Taira E, Hirose M. Mizagliflozin, a selective SGLT1 inhibitor, improves vascular cognitive impairment in a mouse model of small vessel disease. Pharmacol Res Perspect. 2021 Oct;9(5):e00869. doi: 10.1002/prp2.869. PMID: 34586752; PMCID: PMC8480397.
In vitro protocol:
1. Ishida N, Saito M, Sato S, Tezuka Y, Sanbe A, Taira E, Hirose M. Mizagliflozin, a selective SGLT1 inhibitor, improves vascular cognitive impairment in a mouse model of small vessel disease. Pharmacol Res Perspect. 2021 Oct;9(5):e00869. doi: 10.1002/prp2.869. PMID: 34586752; PMCID: PMC8480397.
In vivo protocol:
1. Ishida N, Saito M, Sato S, Tezuka Y, Sanbe A, Taira E, Hirose M. Mizagliflozin, a selective SGLT1 inhibitor, improves vascular cognitive impairment in a mouse model of small vessel disease. Pharmacol Res Perspect. 2021 Oct;9(5):e00869. doi: 10.1002/prp2.869. PMID: 34586752; PMCID: PMC8480397.
1: Song P, Onishi A, Koepsell H, Vallon V. Sodium glucose cotransporter SGLT1 as a therapeutic target in diabetes mellitus. Expert Opin Ther Targets. 2016 Apr 12:1-17. [Epub ahead of print] PubMed PMID: 26998950. 2: Dobbins RL, Greenway FL, Chen L, Liu Y, Breed SL, Andrews SM, Wald JA, Walker A, Smith CD. Selective sodium-dependent glucose transporter 1 inhibitors block glucose absorption and impair glucose-dependent insulinotropic peptide release. Am J Physiol Gastrointest Liver Physiol. 2015 Jun 1;308(11):G946-54. doi: 10.1152/ajpgi.00286.2014. Epub 2015 Mar 12. PubMed PMID: 25767259.

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