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U-73122

Cayman Chemical Item Number 70740

(CAS 112648-68-7)

U-73122 (CAS 112648-68-7)

See more	Inhibitors (493) Phospholipase (79) Immunology (181)

Description

U-73122 is an inhibitor of PLC-dependent processes, however, the mechanism of action remains unclear.^1,2,3 The IC₅₀ values for inhibition of platelet aggregation induced by collagen or thrombin is 0.6 and 5 µM, respectively.² It also exhibits inhibitory activity against HIV-1 integrase with an IC₅₀ value of 7 µM.⁴

1 Smith, R.J., Sam, L.M., Justen, J.M., et al. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: Effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. J Pharmacol Exp Ther 253 688-697 (1990).

2 Bleasdale, J.E., Thakur, N.R., Gremban, R.S., et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther 255 756-768 (1990).

3 Hildebrandt, J., Plant, T.D., and Meves, H. The effects of bradykinin on K+ currents in NG108-15 cells treated with U73122, a phospholipase C inhibitor, or neomycin. Br J Pharmacol 120 841-850 (1997).

4 Burke, T.R., Fesen, M.R., Mazumder, A., et al. Hydroxylated aromatic inhibitors of HIV-1 integrase. J Med Chem 38 4171-4178 (1995).

Formal Name	1-[6-[[(17β)-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione
CAS Number	112648-68-7
Molecular Formula	C₂₉H₄₀N₂O₃
Formula Weight	464.6
Formulation	A crystalline solid
Purity	>99%
Stability	1 year
Storage	Room temperature
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard [H][C@@]12CCC3=CC(OC)=CC=C3[C@@]1([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4N(CCCCCCN5C(C=CC5=O)=O)[H]

Background Reading

Thompson, A.K., Mostafapour, S.P., Denlinger, L.C., et al. The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation. J Biol Chem 266 23856-23862 (1991).

Bleasdale, J.E., Thakur, N.R., Gremban, R.S., et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther 255 756-768 (1990).

Burke, T.R., Fesen, M.R., Mazumder, A., et al. Hydroxylated aromatic inhibitors of HIV-1 integrase. J Med Chem 38 4171-4178 (1995).

Smith, R.J., Sam, L.M., Justen, J.M., et al. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: Effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. J Pharmacol Exp Ther 253 688-697 (1990).

Hildebrandt, J., Plant, T.D., and Meves, H. The effects of bradykinin on K+ currents in NG108-15 cells treated with U73122, a phospholipase C inhibitor, or neomycin. Br J Pharmacol 120 841-850 (1997).

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U-73122 is available in the following screening library:

Bio-active Lipid I Screening Library (96-Well)

Size	Price	Quantity	Subtotal
1 mg	$16.00		$0.00
5 mg	$64.00		$0.00
10 mg	$96.00		$0.00
25 mg	$180.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-11. Prices are subject to change without notice.

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