反应 #554588

ord-6edf2a5ad7274373baa01fed4332c23e

反应方程式

O=P([O-])([O-])[O-].[Na+].[Na+].[Na+]
sodium phosphate
CC(C)[C@@H](CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@H]4C[C@@H](NCCCNCCCCN)CC[C@]4(C)[C@H]3CC[C@]12C)OS(=O)(=O)O.C[C@H](O)C(=O)O
squalamine lactate
O=P([O-])([O-])[O-]
phosphate
CC(C)[C@@H](CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@H]4C[C@@H](NCCCNCCCCN)CC[C@]4(C)[C@H]3CC[C@]12C)OS(=O)(=O)O.C[C@H](O)C(=O)O
squalamine lactate
CC(C)[C@@H](CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@H]4C[C@@H](NCCCNCCCCN)CC[C@]4(C)[C@H]3CC[C@]12C)OS(=O)(=O)O.O=P([O-])([O-])[O-]
squalamine phosphate
CC(C)[C@@H](CC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@H]4C[C@@H](NCCCNCCCCN)CC[C@]4(C)[C@H]3CC[C@]12C)OS(=O)(=O)O.C[C@H](O)C(=O)O
squalamine lactate

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他subject with a syringe
  2. 2
    其他Over the course of the following 24 hours
  3. 3
    workup.WAITThese signs and symptoms persisted for about 1 week

实验过程

A 10 mg/ml solution of squalamine lactate was prepared in 5% dextrose. A squalamine phosphate suspension was prepared by adjusting the 10 mg/ml squalamine lactate solution to 50 mM phosphate by addition of 1M sodium phosphate, pH 7.4. 0.1 ml of each preparation was then separately injected into the subcutaneous space between the thumb and second finger of a healthy human subject with a syringe bearing a 26 gauge needle. Within seconds of injection of the squalamine lactate solution, the subject experienced an intense stinging sensation not unlike an insect sting. This sensation persisted for about 20 minutes. Over the course of the following 24 hours the site became tender, swollen, and visibly red. These signs and symptoms persisted for about 1 week, gradually diminishing in intensity.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08623416B2uspto-grants-2014_01