530821 PTP1B Inhibitor II, JTT-551 - Calbiochem

530821
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₃₄H₄₃N₃O₃S₂•2HCl

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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable, orally available dithiazolylmethylglycinate that acts as a potent, selective, and reversible inhibitor of protein tyrosine phosphatase 1B (PTP1B; Ki = 220 nM). The inhibition appears to be of mixed type. Does not affect the activities of TCPTP, CD45, and LAR phosphatases (Ki = 9.3, > 30 and > 30 µM, respectively). Shown to increase insulin-stimulated glucose uptake in L6 rat skeletal muscle cells (~10-30 µM). Enhances insulin receptor phosphorylation in liver of ob/ob mice and reduces blood glucose level in a dose-dependent manner with hypoglycemic effects evident at > 1 mg/kg (p.o.). Also effective in reducing blood glucose levels in db/db mice (>3 mg/kg, p.o.) without causing any weight gain.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number530821
      Brand Family Calbiochem®
      Synonyms2-(((5-tert-Butylthiazol-2-yl)methyl)((4-(4-((4-heptan-4-yl)phenoxy)methyl)phenyl)thiazol-2-yl)methyl)amino)acetic acid, 2HCl, (((5-(1,1-Dimethylethyl)thiazol-2-yl)methyl)(((4-(4-(4-(1-propylbutyl)phenoxy)methyl)phenl)thiazol-2-yl)methyl)amino)acetic acid, 2HCl, JTT551, Protein Tyrosine Phosphatase 1B Inhibitor II; PTP Inhibitor XVI, PTPN2/TCPTP Inhibitor IV
      References
      ReferencesFukuda, S., et al. 2010. Diabetes Obes. Metab. 12, 299.
      Product Information
      FormOff-white solid
      FormulationSupplied as a diHCl salt.
      Hill FormulaC₃₄H₄₃N₃O₃S₂•2HCl
      Chemical formulaC₃₄H₄₃N₃O₃S₂•2HCl
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPTP1B
      Primary Target K<sub>i</sub>220 nM for PTP1B
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PTP1B Inhibitor II, JTT-551 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Fukuda, S., et al. 2010. Diabetes Obes. Metab. 12, 299.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision09-December-2016 JSW
      Synonyms2-(((5-tert-Butylthiazol-2-yl)methyl)((4-(4-((4-heptan-4-yl)phenoxy)methyl)phenyl)thiazol-2-yl)methyl)amino)acetic acid, 2HCl, (((5-(1,1-Dimethylethyl)thiazol-2-yl)methyl)(((4-(4-(4-(1-propylbutyl)phenoxy)methyl)phenl)thiazol-2-yl)methyl)amino)acetic acid, 2HCl, JTT551, Protein Tyrosine Phosphatase 1B Inhibitor II; PTP Inhibitor XVI, PTPN2/TCPTP Inhibitor IV
      DescriptionA cell-permeable dithiazolylmethylglycinate that acts as a PTP1B-selective tyrosine phosphatase inhibitor (Ki = 220 nM/PTP1B, 9.3 µM/TCPTP, >30 µM/CD45, >30 µM/LAR; Substrate = pNPP, Cat. nos. 6535-OP & 6537-OP) with a mixed-type mode of inhibition. Shown to enhance insulin-stimulated glucose uptake by rat L6 myotubes (by 17% and 36% in 10 min, respectively, at 10 and 30 µM; drug treatment starts 2 h prior to 10 nM insulin stimulation) in vitro and significantly enhance insulin-induced IR tyrosine phosphorylation (1 min) in liver of overnight fasted ob/ob mice (59% vs. 39% of C57BL/6J mice level, respectively, with or without single 10 mg/kg oral dosage 3 h prior to 3 U/kg insulin i.v. injection) in vivo. Daily oral administration is efficacious in reducing blood glucose and triglyceride levels among ob/ob (10 mg/kg/d) and db/db mice (30 mg/kg/d) without significant effect on body weight, while blood insulin level reduction is also seen among ob/ob, but not db/db mice.
      FormOff-white solid
      FormulationSupplied as a diHCl salt.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₄H₄₃N₃O₃S₂•2HCl
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesFukuda, S., et al. 2010. Diabetes Obes. Metab. 12, 299.