TS-021

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

MedKoo CAT#: 528208

CAS#: 667865-69-2

Description: TS-021 is a dipeptidyl peptidase 4 (DPP-4) inhibitor potentially for the treatment of type 2 diabetes. TS-021 and/or metformin significantly improved glucose tolerance and glucagon-like peptide-1 (GLP-1) level, and TS-021 alone or in combination with metformin significantly increased the plasma insulin level after nutrient ingestion. In the chronic treatment study, TS-021 in combination with metformin significantly lowered the glycosylated hemoglobin level, plasma insulin level, and α-cell-to-β-cell area ratio in pancreatic islets. TS-021 exhibited a significant improvement in glucose tolerance by increasing the plasma insulin level during oral glucose tolerance tests.

Chemical Structure

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TS-021
CAS# 667865-69-2
Instruction

Theoretical Analysis

MedKoo Cat#: 528208
Name: TS-021
CAS#: 667865-69-2
Chemical Formula: C17H24FN3O5S
Exact Mass: 0.00
Molecular Weight: 401.453
Elemental Analysis: C, 50.86; H, 6.03; F, 4.73; N, 10.47; O, 19.93; S, 7.99

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 667865-69-2 (sulfonate); 625110-37-4 (free)  

Synonym: TS-021; TS 021; TS021; TS-021 Free

IUPAC/Chemical Name: (2S,4S)-4-fluoro-1-((1-hydroxy-2-methylpropan-2-yl)glycyl)pyrrolidine-2-carbonitrile benzenesulfonate

InChi Key: BMWITAUNXBHIPO-OZZZDHQUSA-N

InChi Code: InChI=1S/C11H18FN3O2.C6H6O3S/c1-11(2,7-16)14-5-10(17)15-6-8(12)3-9(15)4-13;7-10(8,9)6-4-2-1-3-5-6/h8-9,14,16H,3,5-7H2,1-2H3;1-5H,(H,7,8,9)/t8-,9-;/m0./s1

SMILES Code: N#C[C@H]1N(C(CNC(C)(C)CO)=O)C[C@@H](F)C1.O=S(C2=CC=CC=C2)(O)=O

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

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:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 401.45 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:
In vitro protocol:
In vivo protocol:

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1: Tajima A, Hirata T, Taniguchi K, Kondo Y, Kato S, Saito-Hori M, Ishimoto T, Yamamoto K. Combination of TS-021 with metformin improves hyperglycemia and synergistically increases pancreatic β-cell mass in a mouse model of type 2 diabetes. Life Sci. 2011 Oct 24;89(17-18):662-70. doi: 10.1016/j.lfs.2011.08.005. PubMed PMID: 21872612.

2: Tajima A, Yamamoto K, Kozakai A, Okumura-Kitajima L, Mita Y, Kitano K, Jingu S, Nakaike S. (2S,4S)-4-Fluoro-1-{[(2-hydroxy-1,1-dimethylethyl)amino]acetyl}-pyrrolidine-2-car bonitrile monobenzenesulfonate (TS-021) is a selective and reversible dipeptidyl peptidase IV inhibitor. Eur J Pharmacol. 2011 Mar 25;655(1-3):99-107. doi: 10.1016/j.ejphar.2011.01.010. PubMed PMID: 21262219.

3: Fukushima H, Hiratate A, Takahashi M, Mikami A, Saito-Hori M, Munetomo E, Kitano K, Chonan S, Saito H, Suzuki A, Takaoka Y, Yamamoto K. Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors. Bioorg Med Chem. 2008 Apr 1;16(7):4093-106. doi: 10.1016/j.bmc.2008.01.016. PubMed PMID: 18243000.