ChemicalBook > CAS DataBase List > TOFOGLIFLOZIN

TOFOGLIFLOZIN

Product Name: TOFOGLIFLOZIN
CAS No.: 1201913-82-7
Chemical Name: TOFOGLIFLOZIN
Synonyms: Tofogliflozin Monohydrate;CSG452; CSG-452; TOFOGLIFLOZIN; CSG 452; UNII-554245W62TTOFOGLIFLOZIN [INN]; TOFOGLIFLOZIN ANYHYDROUS;Togliflozin;CSG 452(hydrate);Tofogliflozin(CSG452);Tofogliflozin (hydrate);TOFOGLIFLOZIN USP/EP/BP;Tofogliflozin anyhydrous;Tofogliflozin hydrate (1:1);Tofogliflozin Hydrate (JAN)
CBNumber: CB92667680
Molecular Formula: C22H26O6.H2O
Formula Weight: 404.46
MOL File: 1201913-82-7.mol

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TOFOGLIFLOZIN Property

storage temp.: Store at -20°C
solubility: DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH7.2)(1:20): 0.05 mg/ml
form: A crystalline solid
color: White to off-white
InChIKey: ZXOCGDDVNPDRIW-XGKWJGTMNA-N
SMILES: O[C@@H]1[C@H]([C@H](O)[C@@H](CO)O[C@@]21OCC1=CC=C(CC3C=CC(CC)=CC=3)C=C21)O.O |&1:1,2,3,5,9,r|

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23509
Product name: Tofogliflozin (hydrate)
Purity: ≥95%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 23509
Product name: Tofogliflozin (hydrate)
Purity: ≥95%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 23509
Product name: Tofogliflozin (hydrate)
Purity: ≥95%
Packaging: 10mg
Price: $230
Updated: 2024/03/01

Cayman Chemical

Product number: 23509
Product name: Tofogliflozin (hydrate)
Purity: ≥95%
Packaging: 25mg
Price: $420
Updated: 2024/03/01

ChemScene

Product number: CS-3792
Product name: Tofogliflozin(hydrate)
Purity: 98.85%
Packaging: 5mg
Price: $100
Updated: 2021/12/16

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TOFOGLIFLOZIN Chemical Properties,Usage,Production

Description

Tofogliflozin hydrate, which is a sodium-glucose co-transporter 2 inhibitor, was approved in Japan for the treatment of type 2 diabetes at the same time as luseogliflozin hydrate (XIX). The drug was discovered by Chugai Pharmaceutical and jointly developed with Sanofi-Aventis and Kowa. Tofogliflozin hydrate reduces glucose levels by inhibiting the reuptake of glucose by selectively inhibiting SGLT2, and plays a key role in the reuptake of glucose in the proximal tubule of the kidneys.

Uses

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2[1]. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells[2].

Synthesis

Reduction of commercially available 2-bromoterephtalic acid (268) through the use of trimethoxyborane and borane- THF proceeded in 89% yield to afford diol 269. Subjection of this compound to 2-methoxypropene (270) under acidic conditions generated bis-acetonide 271. This bromide then underwent lithium¨Chalogen exchange followed by exposure to magnesium bromide and treatment with lactone 272 (which was prepared by persilylation of commercially available (3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2Hpyran- 2-one (277). This mixture was worked up with aqueous ammonium chloride and upon treatment with p-TsOH in methanol resulted in spiroacetal 273. Next, global protection of all alcohol functionalities within 273 was affected by reaction with methylchloroformate and DMAP in acetonitrile. The benzyl carbonate within 274 was selectively exchanged via Suzuki coupling with 4-ethylphenylboronic acid (275) to afford methylene dibenzyl system 276. Subsequent treatment with aqueous sodium hydroxide in methanol followed by crystallization from 1:6 acetone and water furnished the desired product tofogliflozin hydrate (XXXIV) in 75% yield.

in vivo

Tofogliflozin (0.1-10 mg/kg; oral administration; once daily; for 4 weeks; db/db mice) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice^[1].

Animal Model:	db/db mice^[1]
Dosage:	0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, or 10 mg/kg
Administration:	Oral administration; once daily; for 4 weeks
Result:	Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight.

IC 50

SGLT2

References

[1] Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. DOI:10.1124/jpet.112.191593
[2] Ishibashi Y, et al. Tofogliflozin, A Highly Selective Inhibitor of SGLT2 Blocks Proinflammatory and Proapoptotic Effects of Glucose Overload on Proximal Tubular Cells Partly by Suppressing Oxidative Stress Generation. Horm Metab Res. 2016 Mar;48(3):191-5. DOI:10.1055/s-0035-1555791

TOFOGLIFLOZIN Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from TOFOGLIFLOZIN manufacturers

Wuhan JiyunZen Tech Co., Ltd.

Product: Tofogliflozin 1201913-82-7
Price: US $5.00-0.50/KG
Min. Order: 1KG
Purity: 99% hplc
Supply Ability: 500TONS
Release date: 2025-06-05

Shaanxi Dideu New Materials Co. Ltd

Product: TOFOGLIFLOZIN 1201913-82-7
Price: US $0.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 10000KGS
Release date: 2025-03-11

Qiuxian Baitai New Material Co., LTD

Product: TOFOGLIFLOZIN 1201913-82-7
Price: US $216.00/mg
Min. Order: 1g
Purity: 99.99%
Supply Ability: 5ton/Month
Release date: 2021-12-03

1201913-82-7, TOFOGLIFLOZINRelated Search:

Crizotinib Plx-4032 (RG7024) SERGLIFLOZIN Ertugliflozin L-pyroglutamic acid Tofogliflozin 2,3,4,6-Tetrakis-O-trimethylsilyl-D-gluconolactone Acetoxy Empagliflozin Dexrazoxane Acarbose Gliclazide PF-04971729 Teneligliptin Hydrobromide Pioglitazone hydrochloride Sofosbuvir D-Glucitol, 1,5-dideoxy-1,5-epithio-1-C-[5-[(4-ethoxyphenyl)Methyl]-2-Methoxy-4-Methylphenyl]-, (1S)- Dapagliflozin Empagliflozin Canagliflozin

Tofogliflozin (hydrate)

(1S,3'R,4'S,5'S,6'R)-6-[(4-Ethylphenyl)methyl]-3',4',5',6'-tetrahydro-6'-(hydroxymethyl)spiro[isobenzofuran-1(3H),2'-[2H]pyran]-3',4',5'-triol hydrate (1:1)

Tofogliflozin hydrate (1:1)

Tofogliflozin Monohydrate

Tofogliflozin hydrate (1:1)-API

CSG452; CSG-452; TOFOGLIFLOZIN; CSG 452; UNII-554245W62TTOFOGLIFLOZIN [INN]; TOFOGLIFLOZIN ANYHYDROUS

Tofogliflozin anyhydrous

UNII-554245W62TTofogliflozin [INN]

CSG 452(hydrate)

(3S,3'R,4'S,5'S,6'R)-5-[(4-ethylphenyl)methyl]-6'-(hydroxymethyl)spiro[1H-2-benzofuran-3,2'-oxane]-3',4',5'-triol,hydrate

Tofogliflozin(CSG452)

Tofogliflozin Hydrate (JAN)

Tofogliflozin hydrate (CSG-452 hydrate)

TOFOGLIFLOZIN USP/EP/BP

Togliflozin

Tofogliflozin Monohydrate（CSG 452 hydrate）

(1S,3'R,4'S,5'S,6'R)-6-(4-Ethylbenzyl)-6'-(hydroxymethyl)-3',4',5',6'-tetrahydro-3H-spiro[isobenzofuran-1,2'-pyran]-3',4',5'-triol hydrate

Tofogliflozin (hydrate), 10 mM in DMSO

(1S,3'R,4'S,5'S,6'R)-6-(4-Ethylbenzyl)-6'-(hydroxymethyl)-3',4',5',6'-tetrahydro-3H-spiro[isobenzofuran-1,2'-pyran]-3',4',5'-triol hydrate

1201913-82-7

C22H26O6H2O

API