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531465 Val-boroPro - CAS 150080-09-4 - Calbiochem

Overview

Key Specifications Table

CAS #Empirical Formula
150080-09-4C₁₀H₂₃BN₂O₆S

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      Glass bottle 10 mg
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      Description
      OverviewAn orally available amino boronic acid dipeptide with antihyperglycemic and anticancer properties. Acts as a highly potent, reversible, and transition state analog inhibitor of dipeptidyl peptidase IV (DPP-IV; IC50 = 26 nM; Ki = 180 pM). Also inhibits the activity of other prolyl peptidases (IC50 = 15 nM for DPP-II; and Ki = 1.5 nM and 760 pM for DPP8 and DPP9, respectively) and at much higher concentrations affects the activities of quiescent cell proline dipeptidase (QPP, DPP7; IC50 = 310 nM), PEP (IC50 = 390 nM) and fibroblast activation protein (FAP; IC50 = 560 nM). However, it does not inhibit the activity of trypsin, chymoptrypsin, thrombin, plasmin, tryptase, leukocyte elastase, and plasma kallikrein even at high levels (~100 µM). Promotes hematopoiesis and the growth of primitive hematopoietic progenitor cells by increasing the production of G-CSF, IL-6, and IL-11 by bone marrow stromal cells in mice. Although it has no direct cytotoxic effect on tumors in vitro, but oral administration in mice is shown to reduce the growth of syngeneic tumors derived from fibrosarcoma (WEHI164), lymphoma (EL4 and A20/2J), melanoma (B16-F10), and mastocytoma (P815) cell lines and augments antibody-dependent cell-mediated cytotoxicity. Note: In aqueous physiological solutions, it can cyclize in a time-dependent manner causing a 100-fold diminution in its inhibitory potency. However, at lower pH range it remains in an active open chain form. Maximum tolerated dose in mice or rats is ~ 25 µg/kg.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531465
      Brand Family Calbiochem®
      SynonymsH₂N-(S)-Val-(R)-boroPro-OH, CH₃SO₃H, H-(S)-Val-(R)-boroPro-OH, CH₃SO₃H, Valinyl-L-boroproline, CH₃SO₃H, DPP Inhibitor, PT-100, Talabostat
      References
      ReferencesPoplawski, S.E., et al. 2011, J. Med. Chem. 54, 2022.
      Connolly, B.A., et al. 2008. J. Med. Chem. 51, 6005.
      Lankas, G.R., et al. 2005. Diabetes 54, 2988.
      Cheng, J.D., et al. 2005. Mol. Cancer Ther. 4, 351.
      Adams, S., et al. 2004. Cancer Res. 64, 5471.
      Jones, B., et al. 2003. Blood 102, 1641.
      Coutts, S.J., et al. 1996. J. Med. Chem. 39, 2087.
      Snow, R.J., et al. 1994. J. Am. Chem. Soc. 116, 10860.
      Kelly, T.A., et al. 1993. J. Am. Chem. Soc. 115, 12637.
      Product Information
      CAS number150080-09-4
      FormLight beige solid
      Hill FormulaC₁₀H₂₃BN₂O₆S
      Chemical formulaC₁₀H₂₃BN₂O₆S
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetDPP-IV, DPP8 and DPP9
      Primary Target IC<sub>50</sub>15 nM for DPP-II
      Primary Target K<sub>i</sub>180 pM
      Secondary targetQPP, PEP and FAP
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalog Number GTIN
      5.31465.0001 04055977260328