U73122

製品コードS8011 バッチS801101

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₉H₄₀N₂O₃

分子量

464.64

CAS No.

112648-68-7

Solubility (25°C)*

体外

DMF (warmed with 50ºC water bath)

24 mg/mL (51.65 mM)

DMSO (warmed with 50ºC water bath)

0.01 mg/mL (0.02 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMF 1 40%PEG300 2 5%Tween80 3 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.000mg/ml (2.15mM)

Taking the 1 mL working solution as an example, add 50 μL 20 mg/ml clarified DMF stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. . The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca²⁺ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO).
in vitro	U73122 significantly inhibits aggregation of human platelets induced by a variety of agonists, including collagen, thrombin, ADP, arachidonic acid, with IC50 of 1-5 μM. This compound (10 μM) inhibits the production of IP3 and the subsequent rapid increase in cytosolic Ca²⁺ induced by either thrombin or U-46619 through inhibiting hydrolysis of phosphatidyl[³H]inositol and phosphatldyl[³H]inosito1 4,5-bisphosphate catalyzed by a soluble fraction from platelets (K_i=9 and 40 μM, respectively). It inhibits thromboxane B production induced by collagen through inhibiting receptor-coupled mobilization of arachidonic acid. This chemical inhibits also FMLP-induced aggregation of human polymorphonuclear neutrophils and the associated production of IP3 and diacylglycerol. ^[1] This compound causes a concentration-dependent inhibition of C5a, FMLP, PAF and LTB4-induced MPO and B12-BP release from cyto-chalasin B-treated PMNs. The IC50 values are 60 (FMLP), 110 (LTB4), 115 (C5a) and 120 (PAF) nM for MPO release; and 105 (FMLP), 110 (LTB4), 120 (C5a) and 140 (PAY) nM for B12-BP release. It is also a potent inhibitor of superoxide anion production by cytochalasin B-treated PMNs activated with either C5a or FMLP with IC50 of 160 and 300 nM, respectively. This chemical causes suppression of the rise in [Ca²⁺]_i, IP3 production and DAG production in FMLP-stimulated PMNs with IC50 of 500 nM, 2 μM, and 2 μM, respectively. 3 μM of this compound causes 100% inhibition of FMLP-induced GTPase activity. It causes a concentration-dependent inhibition of the FMLP-evoked association of PKC with the extractable particulate fraction of PMNs, but not a soluble preparation of PMN PKC. ^[2] It significantly inhibits recombinant human PLC-β2, with an IC50 of ~6 μM. This compound has little effect on PLC-β1, PLC-β3, or PLC-β4. It reduces interleukin-8 and leukotriene B4-induced Ca²⁺ flux and chemotaxis in human neutrophils with IC50 of ~6 μM and ~5 μM, respectively. ^[3] 1 μM of this compound blocks bradykinin (BK)-induced increases in the intracellular free Ca²⁺ concentration in undifferentiated NG108-15 cell. The IC50 for a 20-min exposure is approximately 200 nM. 1 μM of this chemical produces a small but significant increase in [Ca²⁺]_i which results from Ca ²⁺ release from an intracellular store. In differentiated NG108-15 cells it blocks completely depolarization-induced Ca²⁺ influx. In contrast, in DRG neurons this compound inhibits only slightly voltage-sensitive Ca²⁺ channels. ^[4] It is a relatively specific inhibitor of G-protein-mediated phospholipase C activation in pancreatic acini. This compound inhibits phosphatidylinositol (PI) hydrolysis on stimulation with either cholecystokinin (by 81%) or carbachol (by 73%) at a maximal effect concentration of 10 μM. This chemical (10 μM) inhibits the increases in [Ca²⁺]_i stimulated by high concentrations of secretagogues in fura-2-loaded acini. It also inhibits the [Ca²⁺]_i signal generated by directly stimulating G-proteins with sodium fluoride. This compound rapidly inhibits the oscillating [Ca²⁺]_i signal elicited by low concentrations of cholecystokinin or carbachol. ^[5] It increases the activity of hPLCβ3 in a concentration-and time-dependent manner in a cell-free micellar system, with up to an 8-fold increase in enzyme activity and a EC50 of 13.6 μM. Activation of hPLCβ3 by this compound requires covalent modification of cysteines. This chemical (10 μM) also activates hPLCγ1(>10-fold) and hPLCβ2(~2-fold); PLC δ1 is neither activated nor inhibited. ^[6]
in vivo	U73122 (30 mg/kg i.p.) blocks swelling of rats hind paw by 65 and 80% at 1 and 3 h postcarrageenan challenge. This compound (0.1 mg/mL) inhibits carrageenan-induced macrophage and lymphocyte accumulation into subcutaneous chambers in dogs by 65 and 74%, respectively. This chemical (30 mg/kg i.p.) totally inhibits the LPS-induced increase in macrophage and lymphocyte infiltration and prostaglandin E2 production (by 80%) in a mouse peritonitis model, and inhibits and 12- O-tetradecanoyl-phorbol-13-acetate-induced ear edema in mice. ^[3]

製品説明

U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca²⁺ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO).

in vitro

U73122 significantly inhibits aggregation of human platelets induced by a variety of agonists, including collagen, thrombin, ADP, arachidonic acid, with IC50 of 1-5 μM. This compound (10 μM) inhibits the production of IP3 and the subsequent rapid increase in cytosolic Ca²⁺ induced by either thrombin or U-46619 through inhibiting hydrolysis of phosphatidyl[³H]inositol and phosphatldyl[³H]inosito1 4,5-bisphosphate catalyzed by a soluble fraction from platelets (K_i=9 and 40 μM, respectively). It inhibits thromboxane B production induced by collagen through inhibiting receptor-coupled mobilization of arachidonic acid. This chemical inhibits also FMLP-induced aggregation of human polymorphonuclear neutrophils and the associated production of IP3 and diacylglycerol. ^[1]

This compound causes a concentration-dependent inhibition of C5a, FMLP, PAF and LTB4-induced MPO and B12-BP release from cyto-chalasin B-treated PMNs. The IC50 values are 60 (FMLP), 110 (LTB4), 115 (C5a) and 120 (PAF) nM for MPO release; and 105 (FMLP), 110 (LTB4), 120 (C5a) and 140 (PAY) nM for B12-BP release. It is also a potent inhibitor of superoxide anion production by cytochalasin B-treated PMNs activated with either C5a or FMLP with IC50 of 160 and 300 nM, respectively. This chemical causes suppression of the rise in [Ca²⁺]_i, IP3 production and DAG production in FMLP-stimulated PMNs with IC50 of 500 nM, 2 μM, and 2 μM, respectively. 3 μM of this compound causes 100% inhibition of FMLP-induced GTPase activity. It causes a concentration-dependent inhibition of the FMLP-evoked association of PKC with the extractable particulate fraction of PMNs, but not a soluble preparation of PMN PKC. ^[2]

It significantly inhibits recombinant human PLC-β2, with an IC50 of ~6 μM. This compound has little effect on PLC-β1, PLC-β3, or PLC-β4. It reduces interleukin-8 and leukotriene B4-induced Ca²⁺ flux and chemotaxis in human neutrophils with IC50 of ~6 μM and ~5 μM, respectively. ^[3]

1 μM of this compound blocks bradykinin (BK)-induced increases in the intracellular free Ca²⁺ concentration in undifferentiated NG108-15 cell. The IC50 for a 20-min exposure is approximately 200 nM. 1 μM of this chemical produces a small but significant increase in [Ca²⁺]_i which results from Ca ²⁺ release from an intracellular store. In differentiated NG108-15 cells it blocks completely depolarization-induced Ca²⁺ influx. In contrast, in DRG neurons this compound inhibits only slightly voltage-sensitive Ca²⁺ channels. ^[4]

It is a relatively specific inhibitor of G-protein-mediated phospholipase C activation in pancreatic acini. This compound inhibits phosphatidylinositol (PI) hydrolysis on stimulation with either cholecystokinin (by 81%) or carbachol (by 73%) at a maximal effect concentration of 10 μM. This chemical (10 μM) inhibits the increases in [Ca²⁺]_i stimulated by high concentrations of secretagogues in fura-2-loaded acini. It also inhibits the [Ca²⁺]_i signal generated by directly stimulating G-proteins with sodium fluoride. This compound rapidly inhibits the oscillating [Ca²⁺]_i signal elicited by low concentrations of cholecystokinin or carbachol. ^[5]

It increases the activity of hPLCβ3 in a concentration-and time-dependent manner in a cell-free micellar system, with up to an 8-fold increase in enzyme activity and a EC50 of 13.6 μM. Activation of hPLCβ3 by this compound requires covalent modification of cysteines. This chemical (10 μM) also activates hPLCγ1(>10-fold) and hPLCβ2(~2-fold); PLC δ1 is neither activated nor inhibited. ^[6]

in vivo

U73122 (30 mg/kg i.p.) blocks swelling of rats hind paw by 65 and 80% at 1 and 3 h postcarrageenan challenge. This compound (0.1 mg/mL) inhibits carrageenan-induced macrophage and lymphocyte accumulation into subcutaneous chambers in dogs by 65 and 74%, respectively. This chemical (30 mg/kg i.p.) totally inhibits the LPS-induced increase in macrophage and lymphocyte infiltration and prostaglandin E2 production (by 80%) in a mouse peritonitis model, and inhibits and 12- O-tetradecanoyl-phorbol-13-acetate-induced ear edema in mice. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Phosphoinositide-specific phospholipase C activity assay
キナーゼアッセイ	Assay mixtures (0.2 mL) contains assay buffer (without leupeptin), CaCl₂ (an amount calculated to produce a Ca-EGTA buffer with the required free Ca²⁺ concentration), platelet soluble fraction (5-15 μg of protein) and 4 nmol of either phosphatidyl[³H]inositol or phosphatidyl[³H]inositol 4,5-bisphosphate. Substrata mixtures consists of either phosphatidyl[³H]inositol (3.4 Ci/mol) plus 1-pahnitoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine (1:0.4 M ratio) or phosphatidyl[³H]inositol4,5-bisphosphate (7 Ci/mol) plus 1-palmitoyl 2-oleoyl-sn-giycero-3-phosphoethanolamine (1:4 M ratio). Substrate mixtures are prepared as l0× suspensions of small unilamellar vesicles by consonication of the lipids in assay buffer (Vibra Cell microprobe sonicator, 75 W, 2 times 60 sec). U-73122 is added to assay mixtures in 2 μL of DMSO. This amount of DMSO has a negligible effect on phospholipase C activity under these conditions. This compound is incubated in glass tubes at 37 ℃ for 10 min and then quenched with 1.6 mL of chloroform/rnethanol/HC1 (1 N) (108:108:25, by vol). After vigorous mixing and centrifugation (500 g for 10 min), a portion (0.7 mL) of the aqueous upper layer (0.9 mL) is transferred to a scintillation vial that contains 10 mL of ACS scintillation fluid. Tritium in water-soluble products (>90% being inositol phosphates) is measured by liquid scintillation spectrornetry. Phosphoinositide hydrolysis under these conditions never exceeds 10% of total added and proceeded at a constant rate throughout the incubation period. Blank values are determined from assay mixtures in which platelet soluble fraction is added after the stopping reagent.
細胞アッセイ	細胞株	Cell-free assays
	濃度	6 µM
	反応時間
	実験の流れ
動物実験	動物モデル	Swiss-Webster mic
	投薬量	30 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/2147038/
https://pubmed.ncbi.nlm.nih.gov/2338654/
https://pubmed.ncbi.nlm.nih.gov/14730005/

https://pubmed.ncbi.nlm.nih.gov/8032885/
https://pubmed.ncbi.nlm.nih.gov/1629184/
https://pubmed.ncbi.nlm.nih.gov/21266572/

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カスタマーフィードバック

: , , Cell Res, 2017, 27(6):748-763

: , , Virus Genes, 2016, 53(2):179-189

: Data from [Data independently produced by , , J Neurosci, 2016, 36(16):4534-48.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

TLR4 endocytosis and endosomal TLR4 signaling are distinct and independent outcomes of TLR4 activation [ EMBO Rep, 2025, 10.1038/s44319-025-00444-2]	PubMed: 40204912
Identification of key genes and immune infiltration mechanisms in limb ischemia-reperfusion injury: a bioinformatics and experimental study [ Front Immunol, 2025, 16:1491928]	PubMed: 40416982
Mg2+ influx mediated by TRPM7 triggers the initiation of muscle stem cell activation [ Sci Adv, 2025, 11(14):eadu0601]	PubMed: 40184450
Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src [ Nat Commun, 2024, 15(1):1300]	PubMed: 38346942
Impaired degradation of PLCG1 by chaperone-mediated autophagy promotes cellular senescence and intervertebral disc degeneration [ Autophagy, 2024, 10.1080/15548627.2024.2395797]	PubMed: 39212196
Bactericidal/permeability-increasing protein instructs dendritic cells to elicit Th22 cell response [ Cell Rep, 2024, 43(3):113929]	PubMed: 38457343
Cell-cell interaction determines cell fate of mesoderm-derived cell in tongue development through Hh signaling [ Elife, 2024, 13e85042]	PubMed: 39392396
U-73122, a phospholipase C inhibitor, impairs lymphocytic choriomeningitis virus virion infectivity [ J Gen Virol, 2024, 105(12)002060]	PubMed: 39688895
Microbial metabolite butyrate promotes anti-PD-1 antitumor efficacy by modulating T cell receptor signaling of cytotoxic CD8 T cell [ Gut Microbes, 2023, 15(2):2249143]	PubMed: 37635362
Microbial metabolite butyrate promotes anti-PD-1 antitumor efficacy by modulating T cell receptor signaling of cytotoxic CD8 T cell [ Gut Microbes, 2023, 15(2):2249143]	PubMed: 37635362

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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