U-73122

SKU: orb1300944

Description

U-73122 is a potent phospholipase C (PLC) inhibitor that suppresses agonist-triggered intracellular calcium mobilization in platelets and polymorphonuclear leukocytes (PMNs). It is widely used in vitro to study calcium signaling pathways in immunology, inflammation, and cardiovascular research.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 112648-68-7
• MW: 464.64
• Purity: 97.98%
• Formula: C₂₉H₄₀N₂O₃
• SMILES: COc1ccc2[C@H]3CC[C@]4(C)[C@H](CC[C@H]4[C@@H]3CCc2c1)NCCCCCCN1C(=O)C=CC1=O
• Target: Phospholipase,Lipoxygenase,Ferroptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1.25 mg/mL (2.69 mM);H2O:< 0.1 mg/mL (insoluble);DMSO:8 mg/mL (17.22 mM)

Bioactivity

• In Vivo:
  U-73122 inhibit the production of thromboxane B induced by collagen, where collagen induces this effect by inhibiting receptor-coupled arachidonic acid transfer. U-73122 also suppresse the aggregation of human polymorphonuclear neutrophils an the associated production of IP3 and diacylglycerol induced by FMLP. It notably inhibit the aggregation of human platelets induced by various agonists, including thrombin, collagen, ADP, and arachidonic acid IC50 of 1-5 µM). Thrombin or U-46619 induce the production of IP3 and a subsequent rapid increase in intracellular Ca2+ by inhibitin the hydrolysis of platelet-soluble components catalyzed phosphatidylinositol [3H]mannose and phosphatidylinositol [3H]bisphosphate 4,5-diphosphate (Ki: 9/40 µM), which is inhibited by 10 µM of U-73122.
• In Vitro:
  At a concentration of 0.1 mg/mL, U73122 inhibit the accumulation of 74% of lymphocytes and 65% of macrophages induced by carrageenan in the subcutaneous cavity of dogs. When administered at 30 mg/kg intraperitoneally (i.p.), U73122 blocks 65% and 80% of carrageenan-induced paw edema in rats 1 hour and 3 hours post-treatment, respectively furthermore , it completely inhibit the infiltration of macrophages and lymphocytes, as well as 80% of prostag andin E2 production, in a mouse model of peritonitis triggered by lipopolysaccharides. U73122 also suppresse the swelling of mouse ears induced by 12-O-tetradecanoylphorbol-13-acetate.
• Cell Research:
  U-73122 is dissolved in DMSO. Agonist-induced production of IP3 in PMN is measured by use o the competitive radiobinding assy. PMN (2 x 106-107) in 0.2 ml of phosphate-buffered saline, pH 7.4 [NaC1 (138 mM), Na2HPO4 (8.1 mM , KH2PO4 (1.5 mM), KCI (2.7 mM), CaCl2 (1.0 mM), MgC12 (1.0 mM) and glucose (0.1%, w/v)] are incubated in conical polypropylene tubes at 37℃n a shaking water bath. U-73122 or U-73343 is added (in 1 μL of DMSO) 3 min befor the addition of agonist, FMLP (0.1 μM) plus cytochalasin B (5 μg/ml). FMLP and cytochalasin B are added in 1 μL Each of DMSO and ethanol, respectively Appropriate Vehicle controls are included in Each experiment. PMN incubation mixtures are quenched wit the addition of 0.07 mL of ice-cold TCA (20%, w/v) and a portion (0.2 ml) o the TCA extract is processed fo the measurement of IP3 by competitive radiobinding as described above for platelets.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Phospholipase, U 73122, U73122, U-73122, PLC, LOX, inhibit, Lipoxygenase, Inhibitor, Ferroptosis

Compound Identifiers

PubChem CID

104794