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Discovery Antibodies/(RS)-(Tetrazol-5-yl)glycine/10 mg/T-205-10 mg

价格
¥1920.00
货号:T-205-10mg
浏览量:127
品牌:Discovery
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商品描述
Cat #: D-110
Alternative Name 3-(4)-Dimethylaminobenzylidine anabaseine
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 364.3
    Purity: >98%
    Effective concentration 0.1-10 µM.
      • DMAB-anabaseine dihydrochloride
    Chemical name 4-[(5,6-Dihydro[2,3"-bipyridin]-3(4H)-ylidene)methyl]-N,N-dimethylbenzenamine dihydrochloride.
    Molecular formula C19H21N3*2HCl.
    CAS No.: 154149-38-9, 32013-69-7.
    Activity DMAB-anabaseine dihydrochloride is a partial agonist of α7 nicotinic acetylcholine receptors (nAChR) and antagonist of α4/β2 nAChR1. It blocks the acetylcholine induced α7 current with IC50 ~5 µM2. DMAB-anabaseine dihydrochloride can also displace isotopic (-)-cytisine and α-bungarotoxin binding to rat brain membranes with high affinity3.
      • Kem, W.R. et al. (1997) J. Pharmacol. Exp. Therap. 283, 979.
      • Weltzin, M.M. et al. (2010) J. Pharmacol. 334, 917.
      • de Fiebre, C.M. et al. (1995) Mol. Pharmacol. 47, 164.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or six months at -20°C.
      • DMAB-anabaseine dihydrochloride
        Alomone Labs DMAB-anabaseine dihydrochloride inhibits α7 nicotinic acetylcholine receptors heterologously expressed in Xenopus oocytes.
        A. Current traces of α7 nicotinic acetylcholine receptor activity at -60 mV holding potential. Currents were elicited by application of 100 µM acetylcholine every 50 seconds. Inhibition of these induced currents was achieved upon perfusion of 1 or 10 µM DMAB-anabaseine dihydrochloride (#D-110) (indicated by horizontal bars). B. Superimposed current responses to the application of either 100 µM acetylcholine (Ach) or 100 µM DMAB-anabaseine dihydrochloride (Ana), demonstrating the partial agonist effect on α7 channels.
    References - Scientific background
    • 1. Kombo, D.C. et al. (2011) Eur. J. Med. Chem. 46, 5625.
    • 2. Papke, R.L. et al. (1994) Giacobini E, Becker R (eds) Alzheimer disease: therapeutic strategies, 206.
    • 3. de Fiebre, C.M. et al. (1995) Mol. Pharmacol. 47, 164.
    • 4. Kem, W.R. et al. (1997) J. Pharmacol. Exp. Therap.  283, 979.
    • 5. Stevens, K.E. et al. (1998) Psychopharmacology 136, 320.
    • 6. Weltzin, M.M. et al. (2010) J. Pharmacol. 334, 917.
      • nAChRs are members of the Cys-loop ligand-gated ion channel superfamily, located both in the peripheral and central nervous systems (PNS and CNS, respectively). These receptors, existing as both homopentameric and heteropentameric transmembrane ion channels, are validated therapeutic targets for various CNS pathologies1.

        DMAB-anabaseine (DMAB), an anabaseine analog, is a selectively partial agonist at α7 receptors which are predominantly found in the CNS2,3. In contrast, DMAB is an antagonist at α3β4, α4β2 and other nicotinic receptors4,5 and blocks the α4β2 current with IC50 ~5 µM6.

    Target nAChR
    receive a 5 mg free trial sample!
    Last update: 23/10/2019

    DMAB-anabaseine dihydrochloride (#D-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Discovery Antibodies的Cyclin dependant kinase 2 (CDK2) is a serine/threonine protein kinase which controls both G1/S and G2/M transitions. CDKs along with cyclins and CDK inhibitors regulate cell cycle progression. Specific cyclins activate different CDKs; in early G1, CDK2 pairs with cyclin E to promote entry into the S phase before switching to partner with cyclin A to drive the cell through S phase. Once activated CDKs phosphorylate downstream proteins to initiate signalling cascades. CDK2 phosphorylates and inactivates the RB1 (pRb) tumour suppressor family of proteins.CDK的活动受到严格控制。CDK2活性可以被包括P21在内的一系列抑制剂抑制。细胞周期失调和增殖控制的丧失与细胞转化和癌症密切相关。CDK2在DNA损伤反应(DDR)中的细胞周期停滞中也似乎起着积极作用,它的抑制作用会阻碍DDR,并使细胞对电离辐射敏感,从而诱导细胞死亡。该抗体与AlexaFluor®488偶联。AlexaFluor®488是一种流行的鲜绿色荧光染料,具有高pH稳定性。
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