ChemicalBook > CAS DataBase List > U-73122

U-73122

Product Name
U-73122
CAS No.
112648-68-7
Chemical Name
U-73122
Synonyms
U-73312;U-73122;CS-1793;CS-2400;U-73122 98%;U 73122;U-73122;U-73122 hydrate;U-73122 USP/EP/BP;U-73122 hydrate(U73122);U-73122 - CAS 112648-68-7 - Calbiochem
CBNumber
CB6237598
Molecular Formula
C29H40N2O3
Formula Weight
464.64
MOL File
112648-68-7.mol
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U-73122 Property

Boiling point:
617.1±55.0 °C(Predicted)
Density 
1.16±0.1 g/cm3(Predicted)
storage temp. 
Keep in dark place,Inert atmosphere,Room temperature
solubility 
ethanol: 0.7 mg/mL
form 
solid
pka
10.69±0.40(Predicted)
color 
off-white
Water Solubility 
Soluble in DMSO, ethanol, or DMF at approx. 0.5mg/ml. May require heating or overnight mixing. Insoluble in water
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 turn pink should be discarded.
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Safety

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26-36
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
U6756
Product name
U-73122 hydrate
Purity
powder
Packaging
5mg
Price
$174
Updated
2024/03/01
Sigma-Aldrich
Product number
662035
Product name
U-73122
Packaging
5mg
Price
$172
Updated
2024/03/01
Alfa Aesar
Product number
J62898
Product name
U-73122, 95%
Packaging
1mg
Price
$42.7
Updated
2023/06/20
Alfa Aesar
Product number
J62898
Product name
U-73122, 95%
Packaging
5mg
Price
$154
Updated
2023/06/20
Cayman Chemical
Product number
70740
Product name
U-73122
Purity
≥95%
Packaging
1mg
Price
$21
Updated
2024/03/01
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U-73122 Chemical Properties,Usage,Production

Description

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

Uses

It is used as a phospholipase C, phospholipase A2, and 5-LO inhibitor. It is also determined that in SK-N-SH neuroblastoma cells, U-73122 inhibits agonist-induced down-regulation of muscarinic receptors. In addition, it is a useful tool to investigate receptor-mediated PI turnover in signal transduction. U-73122 is a potent inhibitor of human neutrophil adhesion to biological surfaces (IC50 = 50 nM) as well as adhesion-dependent granule exocytosis and oxidative burst. U-73343 (sc-201422) is useful as a negative control for investigations of U-73122 phospholipase C antagonism and its cellular consequences.

Definition

ChEBI: An aza-steroid that is 3-O-methyl-17beta-estradiol in which the 17beta-hydroxy group is replaced by a 6-(maleimid-1-yl)hexylamino group. An inibitor of phospholipase C.

Biological Activity

Phospholipase C inhibitor. Inhibits agonist-induced platelet aggregation with IC 50 values of 1-5 μ M. Potently inhibits human polymorphonuclear neutrophil adhesion on biological surfaces (IC 50 < 50 nM) and exhibits antinociceptive activity in vivo .

Biochem/physiol Actions

Inhibits the hydrolysis of PPI to IP3, which leads to a decrease in cytosolic free calcium. Inhibits the coupling of G protein-phospholipase C activation, while remaining unaffected by production of cAMP.

storage

Store at RT

References

1) Bleasdale?et al. (1990),?Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils; J. Pharmacol. Exp. Ther.,?255?756 2) Zholos?et al.?(2004),?Phospholipase C, but not InsP3 or DAG,-dependent activation of the muscarinic receptor-operated cation current in guinea-pig ileal smooth muscle cells; Br. J. Pharmacol.,?141?23 3) Jun?et al. (2004),?Diacylglycerol and its formation by phospholipase C regulate Rab- and SNARE dependent yeast vacuole fusion; J. Biol. Chem. ,279?53186 4) Fernandez-Ulibarri?et al.?(2007),?Diacylglycerol is required for the formation of COPI vesicles in the Golgi-to-ER transport pathway; Mol. Biol. Cell,?18?3250

U-73122 Preparation Products And Raw materials

Raw materials

Preparation Products

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U-73122 Suppliers

3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15848
Advantage
69
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4647
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7553
Advantage
61
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4863
Advantage
58
TargetMol Chemicals Inc.
Tel
021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7934
Advantage
58
Shanghai Macklin Biochemical Co.,Ltd.
Tel
15221275939 15221275939
Fax
021-50706099
Email
shenlinxing@macklin.cn
Country
China
ProdList
15878
Advantage
55
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2989
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51471
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4121
Advantage
55

112648-68-7, U-73122Related Search:


  • U-73122
  • 1-[6-[[(17B)-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL]AMINO]HEXYL]-1H-PYRROLE-2,5-DIONE
  • 1-[6-((17BETA-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL)AMINO)HEXYL]-1H-PYRROLE-2,5-DIONE
  • U-73122 98%
  • 1-[6-[((17β)-3-methoxyestra-1,3,5[10]-trien-17-yl)amino]hexyl]-1h-pyrrole-2,5-dione
  • U-73122 hydrate
  • (17β)-3-Methoxy-17-[6-[(2,5-dihydro-2,5-dioxo-1H-pyrrol)-1-yl]hexylamino]estra-1,3,5(10)-triene
  • 1-[6-[[3-Methoxyestra-1,3,5(10)-triene-17β-yl]amino]hexyl]-1H-pyrrole-2,5-dione
  • U-73312
  • 1-(6-((3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione
  • 1H-Pyrrole-2,5-dione, 1-(6-(((17beta)-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-
  • 1-(6-((8R,9S,13S,14S,17S)-3-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-ylamino)hexyl)-1H-pyrrole-2,5-dione
  • 1-[6-[[(17beta)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione U73122
  • U-73122 hydrate(U73122)
  • U-73122 - CAS 112648-68-7 - Calbiochem
  • CS-1793
  • U 73122;U-73122
  • CS-2400
  • 1H-Pyrrole-2,5-dione, 1-[6-[[(17β)-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-
  • U-73122 USP/EP/BP
  • 112648-68-7
  • 12648-68-7
  • C29H40N2O3xH2O
  • Biochemicals and Reagents
  • BioChemical
  • Enzymes, Inhibitors, and Substrates
  • Enzyme Inhibitors
  • Enzyme Inhibitors by Enzyme
  • Phospholipase A 2
  • P to Q
  • Lipid signaling
  • Inhibitors