Talabostat mesylate

• CAT Number: I009692
• CAS Number: 150080-09-4
• Molecular Formula: C10H23BN2O6S
• Molecular Weight: 310.17
• Purity: ≥95%
• Target: DPP-4
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• SMILES: OB([C@H]1N(C([C@@H](N)C(C)C)=O)CCC1)O.CS(=O)(O)=O

Talabostat mesylate (CAT: I009692) is a small molecule inhibitor of dipeptidyl peptidase IV (DPP-IV), an enzyme involved in the degradation of incretin hormones that regulate glucose metabolism. By inhibiting DPP-IV, talabostat mesylate increases the levels of active incretin hormones, such as glucagon-like peptide-1 (GLP-1), leading to improved glycemic control. Talabostat mesylate has been investigated as a potential treatment for type 2 diabetes mellitus and has shown promising results in preclinical and clinical studies. Additionally, talabostat mesylate has demonstrated immunomodulatory effects by inhibiting pro-inflammatory cytokine production and has been explored for its potential anti-inflammatory and anti-cancer properties.

Reference

1: Eager RM, Cunningham CC, Senzer N, Richards DA, Raju RN, Jones B, Uprichard M,
Nemunaitis J. Phase II trial of talabostat and docetaxel in advanced non-small
cell lung cancer. Clin Oncol (R Coll Radiol). 2009 Aug;21(6):464-72. doi:
10.1016/j.clon.2009.04.007. Epub 2009 Jun 5. PubMed PMID: 19501491.
2: Eager RM, Cunningham CC, Senzer NN, Stephenson J Jr, Anthony SP, O/’Day SJ,
Frenette G, Pavlick AC, Jones B, Uprichard M, Nemunaitis J. Phase II assessment
of talabostat and cisplatin in second-line stage IV melanoma. BMC Cancer. 2009
Jul 30;9:263. doi: 10.1186/1471-2407-9-263. PubMed PMID: 19643020; PubMed Central
PMCID: PMC2731782.
3: Cristillo AD, Galmin L, Restrepo S, Hudacik L, Suschak J, Lewis B,
Draghia-Akli R, Aziz N, Weiss D, Markham P, Pal R. HIV-1 Env vaccine comprised of
electroporated DNA and protein co-administered with Talabostat. Biochem Biophys
Res Commun. 2008 May 23;370(1):22-6. doi: 10.1016/j.bbrc.2008.02.145. Epub 2008
Mar 7. PubMed PMID: 18329382.
4: Narra K, Mullins SR, Lee HO, Strzemkowski-Brun B, Magalong K, Christiansen VJ,
McKee PA, Egleston B, Cohen SJ, Weiner LM, Meropol NJ, Cheng JD. Phase II trial
of single agent Val-boroPro (Talabostat) inhibiting Fibroblast Activation Protein
in patients with metastatic colorectal cancer. Cancer Biol Ther. 2007
Nov;6(11):1691-9. Epub 2007 Aug 14. PubMed PMID: 18032930.