三羟甲基氨基甲烷盐酸盐 → 前列腺素 D2

HRID 6685

反应方程式

HRID 6685 反应方程式
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]

参与物

4

反应物 3

HCID 93573三羟甲基氨基甲烷盐酸盐HCID 5360315氯化镁HCID 6519333(E)-7-[(1R,2R,5S)-5-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-3-oxocyclopentyl]hept-5-enoic acid

产物 1

HCID 448457前列腺素 D2

实验过程

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

后处理

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

来源与证据

ORD记录
ord-3b8414190c404782927a055505deeae4
来源数据集
uspto-grants-2006_08
专利号
US07084136B2

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