Bexagliflozin | EGT-1442 | THR144 | CAS#1118567-05-7

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

MedKoo CAT#: 317103

CAS#: 1118567-05-7 (free base)

Description: Bexagliflozin, also known as EGT1442, is a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. The IC(50) values for EGT1442 against human SGLT1 and SGLT2 are 5.6μM and 2nM, respectively. In normal rats and dogs a saturable urinary glucose excretion was produced with an ED(50) of 0.38 and 0.09mg/kg, respectively. EGT1442 showed favorable properties both in vitro and in vivo and could be beneficial to the management of type 2 diabetic patients.

Chemical Structure

Bexagliflozin

CAS# 1118567-05-7 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 317103
Name: Bexagliflozin
CAS#: 1118567-05-7 (free base)
Chemical Formula: C24H29ClO7
Exact Mass: 464.16
Molecular Weight: 464.940
Elemental Analysis: C, 62.00; H, 6.29; Cl, 7.62; O, 24.09

Price and Availability

Size	Price	Availability
25mg	USD 450	2 Weeks
59mg	USD 750	2 weeks
100mg	USD 1250	2 weeks
200mg	USD 2250	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: THR1442; THR-1442; THR 1442; EGT1442; EGT-1442; EGT 1442; Bexagliflozin

IUPAC/Chemical Name: (3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-cyclopropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol

InChi Key: BTCRKOKVYTVOLU-MLYSRARTSA-N

InChi Code: InChI=1S/C24H29ClO7/c25-19-8-3-15(24-23(29)22(28)21(27)20(13-26)32-24)12-16(19)11-14-1-4-17(5-2-14)30-9-10-31-18-6-7-18/h1-5,8,12,18,20-24,26-29H,6-7,9-11,13H2/t20-,21-,22+,23-,24?/m1/s1

SMILES Code: OC[C@@H](O1)[C@@H](O)[C@H](O)[C@@H](O)C1C2=CC(CC(C=C3)=CC=C3OCCOC4CC4)=C(Cl)C=C2

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	100.0	215.08

Preparing Stock Solutions

The following data is based on the product molecular weight 464.94 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.

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:
In vitro protocol:
In vivo protocol:

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1: Azzam O, Carnagarin R, Lugo-Gavidia LM, Nolde J, Matthews VB, Schlaich MP. Bexagliflozin for type 2 diabetes: an overview of the data. Expert Opin Pharmacother. 2021 Nov;22(16):2095-2103. doi: 10.1080/14656566.2021.1959915. Epub 2021 Jul 29. PMID: 34292100.

2: Hoy SM. Bexagliflozin: First Approval. Drugs. 2023 Apr;83(5):447-453. doi: 10.1007/s40265-023-01848-x. PMID: 36867399.

3: Allegretti AS, Zhang W, Zhou W, Thurber TK, Rigby SP, Bowman-Stroud C, Trescoli C, Serusclat P, Freeman MW, Halvorsen YC. Safety and Effectiveness of Bexagliflozin in Patients With Type 2 Diabetes Mellitus and Stage 3a/3b CKD. Am J Kidney Dis. 2019 Sep;74(3):328-337. doi: 10.1053/j.ajkd.2019.03.417. Epub 2019 May 14. PMID: 31101403; PMCID: PMC10077840.

4: Halvorsen YD, Lock JP, Frias JP, Tinahones FJ, Dahl D, Conery AL, Freeman MW. A 96-week, double-blind, randomized controlled trial comparing bexagliflozin to glimepiride as an adjunct to metformin for the treatment of type 2 diabetes in adults. Diabetes Obes Metab. 2023 Jan;25(1):293-301. doi: 10.1111/dom.14875. Epub 2022 Oct 23. PMID: 36178197.

5: Halvorsen YC, Walford GA, Massaro J, Aftring RP, Freeman MW. A 96-week, multinational, randomized, double-blind, parallel-group, clinical trial evaluating the safety and effectiveness of bexagliflozin as a monotherapy for adults with type 2 diabetes. Diabetes Obes Metab. 2019 Nov;21(11):2496-2504. doi: 10.1111/dom.13833. Epub 2019 Aug 8. PMID: 31297965.

6: Benedict SL, Mahony OM, McKee TS, Bergman PJ. Evaluation of bexagliflozin in cats with poorly regulated diabetes mellitus. Can J Vet Res. 2022 Jan;86(1):52-58. Erratum in: Can J Vet Res. 2023 Apr;87(2):152. PMID: 34975223; PMCID: PMC8697324.

7: Pasqualotto E, Figueiredo Watanabe JM, Gewehr DM, da Silva Maintinguer R, van de Sande-Lee S, de Araujo GN, Leal FS, Pinheiro CEA. Efficacy and safety of bexagliflozin in patients with type 2 diabetes mellitus: A systematic review and meta-analysis. Diabetes Obes Metab. 2023 Jul;25(7):1794-1802. doi: 10.1111/dom.15051. Epub 2023 Apr 3. PMID: 36929659.

8: Patoulias D, Dimosiari A. Meta-analysis Addressing the Cardiovascular Safety of Bexagliflozin in Patients With Type 2 Diabetes Mellitus. Am J Cardiol. 2022 Sep 1;178:178-179. doi: 10.1016/j.amjcard.2022.05.005. Epub 2022 Jun 27. PMID: 35773042.

9: Zhang W, Li X, Ding H, Lu Y, Stilwell GE, Halvorsen YD, Welihinda A. Metabolism and disposition of the SGLT2 inhibitor bexagliflozin in rats, monkeys and humans. Xenobiotica. 2020 May;50(5):559-569. doi: 10.1080/00498254.2019.1654634. Epub 2019 Aug 27. PMID: 31432741.

10: Lin J, Wang S, Wen T, Zhang X. Renal protective effect and safety of sodium- glucose cotransporter-2 inhibitors in patients with chronic kidney disease and type 2 diabetes mellitus: a network meta-analysis and systematic review. Int Urol Nephrol. 2022 Sep;54(9):2305-2316. doi: 10.1007/s11255-022-03117-4. Epub 2022 Feb 8. PMID: 35133574.

11: Halvorsen YD, Lock JP, Zhou W, Zhu F, Freeman MW. A 24-week, randomized, double-blind, active-controlled clinical trial comparing bexagliflozin with sitagliptin as an adjunct to metformin for the treatment of type 2 diabetes in adults. Diabetes Obes Metab. 2019 Oct;21(10):2248-2256. doi: 10.1111/dom.13801. Epub 2019 Jun 30. PMID: 31161692.

12: Halvorsen YD, Walford G, Thurber T, Russell H, Massaro M, Freeman MW. A 12-week, randomized, double-blind, placebo-controlled, four-arm dose-finding phase 2 study evaluating bexagliflozin as monotherapy for adults with type 2 diabetes. Diabetes Obes Metab. 2020 Apr;22(4):566-573. doi: 10.1111/dom.13928. Epub 2019 Dec 11. PMID: 31749238.

13: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Sodium-Glucose Cotransporter-2 (SGLT2) Inhibitors. 2023 Feb 10. PMID: 31643612.

14: Hadd MJ, Bienhoff SE, Little SE, Geller S, Ogne-Stevenson J, Dupree TJ, Scott-Moncrieff JC. Safety and effectiveness of the sodium-glucose cotransporter inhibitor bexagliflozin in cats newly diagnosed with diabetes mellitus. J Vet Intern Med. 2023 May-Jun;37(3):915-924. doi: 10.1111/jvim.16730. Epub 2023 May 6. PMID: 37148170; PMCID: PMC10229323.

15: Bhattacharya S, Rathore A, Parwani D, Mallick C, Asati V, Agarwal S, Rajoriya V, Das R, Kashaw SK. An exhaustive perspective on structural insights of SGLT2 inhibitors: A novel class of antidiabetic agent. Eur J Med Chem. 2020 Oct 15;204:112523. doi: 10.1016/j.ejmech.2020.112523. Epub 2020 Jul 19. PMID: 32717480.

16: Banerjee S, Grobelna A. Sodium-Glucose Cotransporter 2 Inhibitors for the Treatment of Diabetic Nephropathy: A Review of Clinical Effectiveness [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Sep 20. PMID: 31725208.

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