530821 PTP1B Inhibitor II, JTT-551 - Calbiochem

530821
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₄H₄₃N₃O₃S₂•2HCl

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30821.0001
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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, Protein Tyrosine Phosphatase 1B Inhibitor II; PTP Inhibitor XVI, PTPN2/TCPTP Inhibitor IV, (((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
          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
          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, Protein Tyrosine Phosphatase 1B Inhibitor II; PTP Inhibitor XVI, PTPN2/TCPTP Inhibitor IV, (((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
          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.