1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione
1-[6-[[(17B)-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL]AMINO]HEXYL]-1H-PYRROLE-2,5-DIONE
CAS: 112648-68-7
Molecular Formula: C29H40N2O3
1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione - Names and Identifiers
1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione - Physico-chemical Properties
| Molecular Formula | C29H40N2O3 |
| Molar Mass | 464.64 |
| Density | 1.16±0.1 g/cm3(Predicted) |
| Boling Point | 617.1±55.0 °C(Predicted) |
| Water Solubility | Soluble in DMSO, ethanol, or DMF at approx. 0.5mg/ml. May require heating or overnight mixing. Insoluble in water |
| Solubility | ethanol: 0.7 mg/mL |
| Appearance | solid |
| Color | off-white |
| pKa | 10.69±0.40(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
| Stability | Stable for 1 year from date of purchase as supplied. Use caution when storing DMSO solutions. Typically solutions in DMSO can be stored at -20°C for approximately 2 months. However, any solutions that |
| Physical and Chemical Properties | Bioactive U73122 is a potent phospholipase C (PLC) inhibitor, which can reduce the increase of Ca2 + in platelets and neutrophils induced by agonists. U73122 was effective in inhibiting human 5-lipoxygenase (5-LO). |
| In vitro study | U73122 significantly inhibits the aggregation of human platelets induced by various agonists, including collagen, thrombin, ADP, arachidonic acid, with an IC50 of 1-5 μm. Thrombin, or U-46619, dose-dependently inhibits C5a,FMLP by inhibiting phosphatidyl catalyzed by the soluble fraction of platelets [U-73122, PAF and LTB4 induced release of MPO and B12-BP from cytochalasin B- treated PMNs. IC50 values for MPO release were 60 (FMLP),110 (LTB4),115 (C5a) and 120 (PAF) nM; IC50 values for release B12-BP were 105 (FMLP),110 (LTB4),120 (C5a) and 140 (PAY) nM. U-73122 is also a potent inhibitor of superoxide anion production by C5a or FMLP-activated cytochalasin B- treated PMNs with IC50 of 160 and 300 nM, respectively. U-73122 also inhibited [Ca U73122 significantly inhibited recombinant human PLC-β2 with an IC50 of ~ 6 μm in FMLP-stimulated PMNs. U73122 had a weak effect on PLC-β1,PLC-β3, or PLC-β4. In human neutrophils, U73122 reduces interleukin-8 and leukotriene b4-induced Ca in undifferentiated NG108-15 cells, 1 μm U73122 blocks bradykinin (BK) the induced intracellular free Ca U73122 is a relatively specific inhibitor of G protein-mediated phospholipase C activation in pancreatic vesicles. U73122 inhibited the hydrolytic action of phosphatidylinositol (PI) on stimulation by Cholecystokinin (81%) or acetylcholine (73%) at a maximum concentration of 10 μm. In fura-2 loaded acini, U73122 (10 μm) inhibited high-concentration secretagogue-stimulated [Ca U73122 concentration-and time-dependently increased the activity of hPLCβ3 in the cell-free micelle system, with an up to 8-fold increase in enzyme activity, the EC50 was 13.6 μm. Activation of HPLC β3 by U73122 requires covalent modification of cysteine. U73122 (10 μm) also activates hPLCγ1(>10-fold) and hPLCβ2(~ 2-fold); Plc1 is not activated or inhibited. |
| In vivo study | U73122 (30 mg/kg, I. P.) blocked the edema of hind paws 65% and 80% of rats after 1 hour and 3 hours of carrageenan treatment. In dogs, U73122 (0.1 mg/ml) inhibited carrageenan-induced accumulation of 65% of macrophages and 74% of lymphocytes into the subcutaneous compartment, respectively. U73122 (30 mg/kg, I. P.) completely inhibited LPS-induced macrophage and lymphocyte infiltration, as well as prostaglandin E2(80%) in a mouse peritonitis model, it also inhibited the mouse ear swelling induced by 12-o-tetradecyl-phorbol -13-acetate. |
1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.152 ml | 10.761 ml | 21.522 ml |
| 5 mM | 0.43 ml | 2.152 ml | 4.304 ml |
| 10 mM | 0.215 ml | 1.076 ml | 2.152 ml |
| 5 mM | 0.043 ml | 0.215 ml | 0.43 ml |
Last Update：2024-01-02 23:10:35
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Product Name: U 73122 Request for quotation
CAS: 112648-68-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 112648-68-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: U-73122 hydrate Visit Supplier Webpage Request for quotationCAS: 112648-68-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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