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MedKoo Cat#: 510330 | Name: T-1095
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Description:

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

T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs). T-1095 may be a useful antidiabetic drug. Long-term treatment with T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats. Chronic administration of T-1095 (0.1% w w(-1) pellet chow, for 12 weeks) decreased blood glucose and haemoglobin A(1C) levels, and improved glucose intolerance in db/db mice. The age-related decrease in plasma insulin levels was markedly inhibited and there was a 2.5 fold increase of insulin content in the pancreas of T-1095-treated db/db mice. T-1095 improved the metabolic abnormalities and inhibit the development of diabetic complications in db/db mice.

Chemical Structure

T-1095
T-1095
CAS#209746-59-8 (T-1095)

Theoretical Analysis

MedKoo Cat#: 510330

Name: T-1095

CAS#: 209746-59-8 (T-1095)

Chemical Formula: C26H28O11

Exact Mass: 516.1632

Molecular Weight: 516.49

Elemental Analysis: C, 60.46; H, 5.46; O, 34.07

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 4,250.00 Ready to ship
2g USD 6,750.00 Ready to ship
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Related CAS #
209746-59-8 (T-1095) 209746-56-5 (T-1095A);
Synonym
T1095, T 1095, T1095
IUPAC/Chemical Name
((2R,3S,4S,5R,6S)-6-(2-(3-(benzofuran-5-yl)propanoyl)-3-hydroxy-5-methylphenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-yl)methyl methyl carbonate
InChi Key
BXNCIERBDJYIQT-PRDVQWLOSA-N
InChi Code
InChI=1S/C26H28O11/c1-13-9-17(28)21(16(27)5-3-14-4-6-18-15(11-14)7-8-34-18)19(10-13)36-25-24(31)23(30)22(29)20(37-25)12-35-26(32)33-2/h4,6-11,20,22-25,28-31H,3,5,12H2,1-2H3/t20-,22-,23+,24-,25-/m1/s1
SMILES Code
O=C(C1=C(O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](COC(OC)=O)O2)O)O)O)C=C(C)C=C1O)CCC3=CC=C(OC=C4)C4=C3
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
Biological target:
T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs).
In vitro activity:
TBD
In vivo activity:
The effects of T-1095, an orally active inhibitor of Na(+)-glucose cotransporter (SGLT), on the development and severity of diabetes in Goto-Kakizaki (GK) rat, a spontaneous, non-obese model of type 2 diabetes, were examined. T-1095 treatment significantly decreased both blood glucose and hemoglobin A(1C) levels in the GK rats. The concomitant increase of urinary glucose excretion indicated that the hypoglycemic action of T-1095 is derived from the enhancement of urinary glucose disposal. Although food intake was not changed in the T-1095-treated rats, the body weight gain was retarded. T-1095 treatment partially ameliorated oral glucose tolerance but not the impaired glucose-induced insulin secretion. Homeostasis model assessment (HOMA) indicated the existence of insulin resistance in GK rats and a significant restoration by T-1095-treatment. There was a reduction of the thermal response in tail-flick testing following long-term hyperglycemia (diabetic neuropathy). Treatment of T-1095 significantly prevented the development of diabetic neuropathy in male GK rats. Sustained improvement of hyperglycemia and prevention of diabetic neuropathy by the T-1095-treatment provide further support the use of SGLT inhibitors for the treatment of diabetes. Reference: Life Sci. 2005 Apr 22;76(23):2655-68. https://www.sciencedirect.com/science/article/abs/pii/S0024320505000640?via%3Dihub

Preparing Stock Solutions

The following data is based on the product molecular weight 516.49 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. Oku A, Ueta K, Arakawa K, Kano-Ishihara T, Matsumoto M, Adachi T, Yasuda K, Tsuda K, Saito A. Antihyperglycemic effect of T-1095 via inhibition of renal Na+-glucose cotransporters in streptozotocin-induced diabetic rats. Biol Pharm Bull. 2000 Dec;23(12):1434-7. doi: 10.1248/bpb.23.1434. PMID: 11145172. 2. Ueta K, Ishihara T, Matsumoto Y, Oku A, Nawano M, Fujita T, Saito A, Arakawa K. Long-term treatment with the Na+-glucose cotransporter inhibitor T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats. Life Sci. 2005 Apr 22;76(23):2655-68. doi: 10.1016/j.lfs.2004.09.038. PMID: 15792833.
In vitro protocol:
TBD
In vivo protocol:
1. Oku A, Ueta K, Arakawa K, Kano-Ishihara T, Matsumoto M, Adachi T, Yasuda K, Tsuda K, Saito A. Antihyperglycemic effect of T-1095 via inhibition of renal Na+-glucose cotransporters in streptozotocin-induced diabetic rats. Biol Pharm Bull. 2000 Dec;23(12):1434-7. doi: 10.1248/bpb.23.1434. PMID: 11145172. 2. Ueta K, Ishihara T, Matsumoto Y, Oku A, Nawano M, Fujita T, Saito A, Arakawa K. Long-term treatment with the Na+-glucose cotransporter inhibitor T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats. Life Sci. 2005 Apr 22;76(23):2655-68. doi: 10.1016/j.lfs.2004.09.038. PMID: 15792833.
1: Helvacı Ö, Helvacı B. A Story of Serendipities: From Phlorizin to Gliflozins. Exp Clin Transplant. 2023 Jun;21(Suppl 2):105-108. doi: 10.6002/ect.IAHNCongress.25. PMID: 37496357. 2: Connelly KA, Zhang Y, Desjardins JF, Thai K, Gilbert RE. Dual inhibition of sodium-glucose linked cotransporters 1 and 2 exacerbates cardiac dysfunction following experimental myocardial infarction. Cardiovasc Diabetol. 2018 Jul 7;17(1):99. doi: 10.1186/s12933-018-0741-9. PMID: 29981571; PMCID: PMC6035399. 3: Miyamoto L, Tsuchiya K. [Sodium-Glucose Transporters as a Therapeutic Target for Diabetes from the Viewpoint of Drug Discovery and Pharmacotherapy]. Yakugaku Zasshi. 2018;138(7):933-938. Japanese. doi: 10.1248/yakushi.17-00223-1. PMID: 29962472. 4: Yamaguchi K, Kato M, Ozawa K, Kawai T, Yata T, Aso Y, Ishigai M, Ikeda S. Pharmacokinetic and pharmacodynamic modeling for the effect of sodium-glucose cotransporter inhibitors on blood glucose level and renal glucose excretion in db/db mice. J Pharm Sci. 2012 Nov;101(11):4347-56. doi: 10.1002/jps.23302. Epub 2012 Aug 23. PMID: 22927193. 5: Nomura S, Sakamaki S, Hongu M, Kawanishi E, Koga Y, Sakamoto T, Yamamoto Y, Ueta K, Kimata H, Nakayama K, Tsuda-Tsukimoto M. Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus. J Med Chem. 2010 Sep 9;53(17):6355-60. doi: 10.1021/jm100332n. PMID: 20690635. 6: Nomura S. Renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for new anti-diabetic agent. Curr Top Med Chem. 2010;10(4):411-8. doi: 10.2174/156802610790980567. PMID: 20180760. 7: von Lewinski D, Gasser R, Rainer PP, Huber MS, Wilhelm B, Roessl U, Haas T, Wasler A, Grimm M, Bisping E, Pieske B. Functional effects of glucose transporters in human ventricular myocardium. Eur J Heart Fail. 2010 Feb;12(2):106-13. doi: 10.1093/eurjhf/hfp191. PMID: 20083620. 8: Isaji M. Sodium-glucose cotransporter inhibitors for diabetes. Curr Opin Investig Drugs. 2007 Apr;8(4):285-92. PMID: 17458177. 9: Fujimoto Y, Torres TP, Donahue EP, Shiota M. Glucose toxicity is responsible for the development of impaired regulation of endogenous glucose production and hepatic glucokinase in Zucker diabetic fatty rats. Diabetes. 2006 Sep;55(9):2479-90. doi: 10.2337/db05-1511. PMID: 16936196. 10: Ueta K, Yoneda H, Oku A, Nishiyama S, Saito A, Arakawa K. Reduction of renal transport maximum for glucose by inhibition of NA(+)-glucose cotransporter suppresses blood glucose elevation in dogs. Biol Pharm Bull. 2006 Jan;29(1):114-8. doi: 10.1248/bpb.29.114. PMID: 16394522. 11: Ueta K, Ishihara T, Matsumoto Y, Oku A, Nawano M, Fujita T, Saito A, Arakawa K. Long-term treatment with the Na+-glucose cotransporter inhibitor T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats. Life Sci. 2005 Apr 22;76(23):2655-68. doi: 10.1016/j.lfs.2004.09.038. PMID: 15792833. 12: Asano T, Ogihara T, Katagiri H, Sakoda H, Ono H, Fujishiro M, Anai M, Kurihara H, Uchijima Y. Glucose transporter and Na+/glucose cotransporter as molecular targets of anti-diabetic drugs. Curr Med Chem. 2004 Oct;11(20):2717-24. doi: 10.2174/0929867043364360. PMID: 15544472. 13: Saito A, Seiyaku T, Tsujihara K. [SGLT inhibitor (T-1095)]. Nihon Rinsho. 2002 Sep;60 Suppl 9:588-93. Japanese. PMID: 12387055. 14: Nunoi K, Yasuda K, Adachi T, Okamoto Y, Shihara N, Uno M, Tamon A, Suzuki N, Oku A, Tsuda K. Beneficial effect of T-1095, a selective inhibitor of renal Na+-glucose cotransporters, on metabolic index and insulin secretion in spontaneously diabetic GK rats. Clin Exp Pharmacol Physiol. 2002 May- Jun;29(5-6):386-90. doi: 10.1046/j.1440-1681.2002.03671.x. PMID: 12010180. 15: Yasuda K, Okamoto Y, Nunoi K, Adachi T, Shihara N, Tamon A, Suzuki N, Mukai E, Fujimoto S, Oku A, Tsuda K, Seino Y. Normalization of cytoplasmic calcium response in pancreatic beta-cells of spontaneously diabetic GK rat by the treatment with T-1095, a specific inhibitor of renal Na+-glucose co- transporters. Horm Metab Res. 2002 Apr;34(4):217-21. doi: 10.1055/s-2002-26714. PMID: 11987033. 16: Oku A, Nawano M, Ueta K, Fujita T, Umebayashi I, Arakawa K, Kano-Ishihara T, Saito A, Anai M, Funaki M, Kikuchi M, Oka Y, Asano T. Inhibitory effect of hyperglycemia on insulin-induced Akt/protein kinase B activation in skeletal muscle. Am J Physiol Endocrinol Metab. 2001 May;280(5):E816-24. doi: 10.1152/ajpendo.2001.280.5.E816. PMID: 11287365. 17: Arakawa K, Ishihara T, Oku A, Nawano M, Ueta K, Kitamura K, Matsumoto M, Saito A. Improved diabetic syndrome in C57BL/KsJ-db/db mice by oral administration of the Na(+)-glucose cotransporter inhibitor T-1095. Br J Pharmacol. 2001 Jan;132(2):578-86. doi: 10.1038/sj.bjp.0703829. PMID: 11159708; PMCID: PMC1572576. 18: Oku A, Ueta K, Arakawa K, Kano-Ishihara T, Matsumoto M, Adachi T, Yasuda K, Tsuda K, Saito A. Antihyperglycemic effect of T-1095 via inhibition of renal Na+-glucose cotransporters in streptozotocin-induced diabetic rats. Biol Pharm Bull. 2000 Dec;23(12):1434-7. doi: 10.1248/bpb.23.1434. PMID: 11145172. 19: Oku A, Ueta K, Arakawa K, Kano-Ishihara T, Matsumoto T, Adachi T, Yasuda K, Tsuda K, Ikezawa K, Saito A. Correction of hyperglycemia and insulin sensitivity by T-1095, an inhibitor of renal Na+-glucose cotransporters, in streptozotocin- induced diabetic rats. Jpn J Pharmacol. 2000 Nov;84(3):351-4. doi: 10.1254/jjp.84.351. PMID: 11138738. 20: Adachi T, Yasuda K, Okamoto Y, Shihara N, Oku A, Ueta K, Kitamura K, Saito A, Iwakura I, Yamada Y, Yano H, Seino Y, Tsuda K. T-1095, a renal Na+-glucose transporter inhibitor, improves hyperglycemia in streptozotocin-induced diabetic rats. Metabolism. 2000 Aug;49(8):990-5. doi: 10.1053/meta.2000.7729. PMID: 10954015. 1198.