530796 TNF-TNFR Interaction Modulator, C87 - Calbiochem

530796
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₁₅ClN₆O₃S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30796.0001
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          Glass bottle 10 mg
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          Description
          OverviewA phenylhydrazonodihydropyrazolone compound that inhibits TNFα/β-stimulated biological activity by modulating, but not abolishing, TNF-TNFR interaction via direct TNF affinity interaction (KD = 110 nM). Shown to prevent murine L929 cell death following hTNFα/β (1 ng/mL; Cat. Nos. 654205 & 654215) and actinomycin D (1 µg/mL; Cat. Nos. 114666 & 2472-OP) treatment (EC50 = 8.73 µM) by blocking TNF/ActD-induced caspase-3/8 cleavages & IκBα degradation without affecting Fas- (CD95) mediated Jurkat cell death or VP-16 (Etoposide; Cat. No. 341205) and ADR (Adriamycin/Doxorubicin; Cat. No. 324380) cytotoxicity in L292 cultures. When applied prior to D-galactosamine (1.2 g D-GalN/kg, Cat. No. 34539) & Lipopolysaccharide (LPS; 50 µg/kg) injection, C87 effectively prevents D-GalN/LPS-induced upregulation of plasma alanine transaminase & aspartate transaminase (ALT & AST) activity, resulting in significantly reduced liver damage and much improved survival rate (3X 12.5 mg C87/kg i.p. dosings 16, 8, & 1 h prior to D-GalN/LPS injection) in a murine hepatitis model in vivo.
          Catalogue Number530796
          Brand Family Calbiochem®
          Synonyms(E)-4-(2-(4-Chloro-3-nitrophenyl)hydrazono)-3-phenyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one, (E)-4-(2-(4-Chloro-3-nitrophenyl)), TNF-TNFR Signaling Inhibitor IV
          References
          ReferencesMa, L., et al. 2014. J. Biol. Chem. 289, 12457.
          Product Information
          FormDark red solid
          Hill FormulaC₂₄H₁₅ClN₆O₃S
          Chemical formulaC₂₄H₁₅ClN₆O₃S
          ReversibleY
          Applications
          Biological Information
          Primary TargetTNFα
          Primary Target K<sub>i</sub>110 nM for hTNF&alpha
          Purity≥97% 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

          TNF-TNFR Interaction Modulator, C87 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Ma, L., et al. 2014. J. Biol. Chem. 289, 12457.
          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.

          Revision19-August-2014 JSW
          Synonyms(E)-4-(2-(4-Chloro-3-nitrophenyl)hydrazono)-3-phenyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one, (E)-4-(2-(4-Chloro-3-nitrophenyl)), TNF-TNFR Signaling Inhibitor IV
          DescriptionA phenylhydrazonodihydropyrazolone compound that inhibits TNFα/β-stimulated biological activity by modulating, but not abolishing, TNF-TNFR interaction via direct TNF affinity interaction (KD = 110 nM in binding study using hTNFα). Shown to prevent murine L929 cell death following hTNFα/β (1 ng/mL; Cat. Nos. 654205 & 654215) and actinomycin D (1 µg/mL; Cat. Nos. 114666 & 2472-OP) treatment (EC50 = 8.73 µM by MTT assay; 20 h TNF/ActD treatment) by blocking TNF/ActD-induced caspase-3/8 cleavages & IκBα degradation without affecting Fas- (CD95) mediated Jurkat cell death or VP-16 (Etoposide; Cat. No. 341205) and ADR (Adriamycin/Doxorubicin; Cat. No. 324380) cytotoxicity in L292 cultures. When applied prior to D-galactosamine (1.2 g D-GalN/kg, Cat. No. 34539) & Lipopolysaccharide (LPS; 50 µg/kg) injection, C87 effectively prevents D-GalN/LPS-induced upregulation of plasma alanine transaminase & aspartate transaminase (ALT & AST) activity, resulting in significantly reduced liver damage and much improved survival rate (58.5% vs. 20.8% with or without 3X 12.5 mg C87/kg i.p. dosings 16, 8, & 1 h prior to D-GalN/LPS injection) in a murine hepatitis model in vivo. A slow and long-lasting (>12 h) JNK T183/Y185 phosphorylation is induced upon TNFα stimulation in L929 cultures, while a much faster and more transient, albeit robust, TNFα-induced JNK pT183/Y185 is seen in the presence of C87 or a TNFα neutralizing antibody.
          FormDark red solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₄H₁₅ClN₆O₃S
          Purity≥97% by HPLC
          SolubilityDMSO (5 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
          ReferencesMa, L., et al. 2014. J. Biol. Chem. 289, 12457.