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Tocris/NBI 35965 hydrochloride/3100/10/10 mg
  • Tocris/NBI 35965 hydrochloride/3100/10/10 mg

Tocris/NBI 35965 hydrochloride/3100/10/10 mg

价格: ¥2460.00 市场价: 4100.00

货号: 3100/10
品牌: Tocris
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    • Description: Potent and selective CRF1 antagonist
      Chemical Name: (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride
      Purity: ≥98% (HPLC)
      Biological Activity Technical Data Solubility Calculators Datasheets References

      Biological Activity

      Potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist (Ki values are 4 and > 10000 nM at CRF1 and CRF2 respectively). Inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50 values are 7.1 and 6.9 respectively) and attenuates CRF and ACTH production in vivo. Orally active and brain penetrant with anxiolytic activity.

      Technical Data

      M. Wt 437.79
      Formula C21H22Cl2N4.HCl
      Storage Desiccate at RT
      Purity ≥98% (HPLC)
      CAS Number 1782228-59-4
      PubChem ID 71433630
      InChI Key LNYUWBPFYXPUIO-RSAXXLAASA-N
      Smiles CC[C@@H]3N(CC5CC5)C1=C2C(C(C4=CC=C(Cl)C=C4Cl)=NN2C3)=NC(C)=C1.Cl

      The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

      All Tocris products are intended for laboratory research use only.

      Solubility Data

      Solvent Max Conc. mg/mL Max Conc. mM
      Solubility
      DMSO 43.78 100
      water 43.78 100

      Preparing Stock Solutions

      The following data is based on the product molecular weight 437.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

      Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
      1 mM 2.28 mL 11.42 mL 22.84 mL
      5 mM 0.46 mL 2.28 mL 4.57 mL
      10 mM 0.23 mL 1.14 mL 2.28 mL
      50 mM 0.05 mL 0.23 mL 0.46 mL

      Product Datasheets

      Certificate of Analysis / Product Datasheet
      Safety Datasheet

      References

      References are publications that support the products' biological activity.

      Million et al (2003) A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats. Brain Res. 985 32 PMID: 12957366

      Hoare et al (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists. Mol.Pharmacol. 63 751 PMID: 12606786

      Gross et al (2005) Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J.Med.Chem. 48 5780 PMID: 16134945


      Keywords: NBI 35965 hydrochloride, supplier, NBI35965, CRF1R, CRF, 1, receptor, antagonist, corticotropin-releasing, factor, 1, antagonists, CRF1, Receptors, CRF1, Receptors, Tocris Bioscience

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