530985 | MICAL-2 Inhibitor II, CCG-203971 - CAS 1443437-74-8 - Calbiochem

530985
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      概要

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      Empirical FormulaCAS #
      C₂₃H₂₁ClN₂O₃ 1443437-74-8

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      5.30985.0001
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          ガラスビン 10 mg
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          Description
          OverviewA cell-permeable, bioavailable, conformationally restricted form of CCG-1423 (Cat. No. 555558) that exhibits enhanced potency (IC50 = 4.2 µM vs 16.6 µM for PC-3 cell migration), but reduced off-target toxicity (IC50 > 100 µM in PC3 cells). Selectively represses sclerodermal fibroblasts proliferation without affecting normal cells (~30 µM). Shown to be more effective in reducing MRTF/SRF-regulated gene transcriptional signaling than Y-27632 (Cat. No. 688000). Suppresses Rho/MRTF/SRF-regulated fibrotic gene expression in primary dermal fibroblasts derived from systemic sclerosis patients in a dose-dependent manner and reverses myofibroblast phenotype in TGFβ-stimulated normal dermal fibroblasts. Blocks MRTF nuclear localization by interfering with the microtubule associated monooxygenase, calponin and LIM domain containing 2 (MICAL-2), mediated regulation of intranuclear actin polymerization. Although exhibits a short in-vivo half-life (~25 min), at higher dosage effectively prevents bleomycin-induced fibrosis in C57BL/6J mice (100 mg/kg, i.p., b.i.d.).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number530985
          Brand Family Calbiochem®
          SynonymsN-(4-Chlorophenyl)-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide, CCG 203971, MLK1 Nuclear Translocation Inhibitor II
          References
          ReferencesHaak, A.J., et al. 2014. J. Pharmacol. Exp. Ther. 349, 480.
          Johnson, L.A., et al. 2014. Inflamm. Bowel Dis. 20, 154.
          Bell, J.L., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3826.
          Product Information
          CAS number1443437-74-8
          FormOff-white powder
          Hill FormulaC₂₃H₂₁ClN₂O₃
          Chemical formulaC₂₃H₂₁ClN₂O₃
          ReversibleY
          Applications
          Biological Information
          Primary TargetMICAL-2
          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

          (M)SDS

          タイトル

          英語版製品安全データシート((M)SDS) 

          参考資料

          参考資料の概要
          Haak, A.J., et al. 2014. J. Pharmacol. Exp. Ther. 349, 480.
          Johnson, L.A., et al. 2014. Inflamm. Bowel Dis. 20, 154.
          Bell, J.L., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3826.
          データシート

          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.

          Revision29-August-2014 JSw
          SynonymsN-(4-Chlorophenyl)-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide, CCG 203971, MLK1 Nuclear Translocation Inhibitor II
          DescriptionA cell-permeable nipecotic bis(amide), chemically modified from CCG-1423 (Cat. No. 555558) for reduced toxicity (non-toxic up to 100 µM in PC-3 cultures and 100 mg/kg/d in mice via i.p.), that effectively downregulates SRF/MLK1 (MRTF-A) target genes mRNA level in primary dermal fibroblast cultures from SSc (systemic sclerosis) patients (IC50 ≤30 µM post 24 h incubation) as well as in LPA-stimulated NIH 3T3 fibroblasts (IC50 = 1 - 3 µM; drug added 23 h prior to 1 h 10 µM LPA stimulation). Likewise, 3-day 10 µM CCG-203971 treatment is shown to reduce cellular α-SMA (α smooth muscle actin) protein and proliferation of SSc dermal fibroblasts to the same level as seen in dermal fibroblasts from healthy donors as well as to prevent 10 ng/mL TGFβ-induced α-SMA upregulation in normal dermal fibroblasts. When administered via intraperitoneal injection (100 mg/50 µL DMSO/kg/12 h), CCG-203971 is reported to be efficacious in preventing bleomycin-(100 µg/µL/1 cm2 skin/animal/day s.c.) induced skin fibrosis in mice (skin thickness = 1.9- vs. 3.5-fold of control, with or without drug treatment at the end of 2-wk induction period) in vivo.
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1443437-74-8
          Chemical formulaC₂₃H₂₁ClN₂O₃
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml)
          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
          ReferencesHaak, A.J., et al. 2014. J. Pharmacol. Exp. Ther. 349, 480.
          Johnson, L.A., et al. 2014. Inflamm. Bowel Dis. 20, 154.
          Bell, J.L., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3826.