Tromethamine hydrochloride → Prostaglandin D2

HRID 565618Notes

Reaction equation

HRID 565618 reaction equation
C(O)C(N)(CO)CO.Cl.[Mg+2].[Cl-].[Cl-].[CH3:13][CH2:14][CH2:15][CH2:16][CH2:17][C@H:18]([OH:37])/[CH:19]=[CH:20]/[C@H:21]1[C:25](=[O:26])[CH2:24][C@H:23]([OH:27])[C@@H:22]1[CH2:28]/[CH:29]=[CH:30]/[CH2:31][CH2:32][CH2:33][C:34]([OH:36])=[O:35]>>[CH3:13][CH2:14][CH2:15][CH2:16][CH2:17][C@H:18]([OH:37])/[CH:19]=[CH:20]/[C@H:21]1[C:25](=[O:26])[CH2:24][C@H:23]([OH:27])[C@@H:22]1[CH2:28]/[CH:29]=[CH:30]\[CH2:31][CH2:32][CH2:33][C:34]([OH:36])=[O:35]

Participants

4

Reactant 3

HCID 93573Tromethamine hydrochlorideHCID 5360315Magnesium ChlorideHCID 6519333(E)-7-[(1R,2R,5S)-5-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-3-oxocyclopentyl]hept-5-enoic acid

Product 1

HCID 448457Prostaglandin D2

Procedure

To a binding-reaction solution (50 mM Tris/HCl, pH 7.4, 5 mM MgCl2) (0.2 ml) were added human platelet membrane fraction (0.1 mg) and 5 nM [3H]PGD2 (115Ci/mmol), and reacted at 4° C. for 90 min. After the reaction completed, the reaction mixture was filtered through the glass fiber filter paper, washed several times with cooled saline, and measured radioactivity retained on the filter paper. The specific binding was calculated by subtracting the non-specific binding (the binding in the presence of 10 μM PGD2) from the total binding. The binding-inhibitory activity of each compound was expressed as concentration required for 50% inhibition (IC50), which was determined by depicting a substitution curve by plotting the binding ratio (%) in the presence of each compound, where the binding ratio in the absence of a test compound is 100%. The results are shown in Table below.

Workup

  1. customreacted at 4° C. for 90 min
  2. filtrationthe reaction mixture was filtered through the glass fiber
  3. filtrationfilter paper
  4. washwashed several times
  5. temperaturewith cooled saline
  6. concentrationThe binding-inhibitory activity of each compound was expressed as concentration

Sources & evidence

ORD record
ord-57997d1a926c4906a2673ed20f5ffceb
Source dataset
uspto-grants-2001_01
Patent number
US06172113B2

Reaction notes

Loading…