ChemicalBook > CAS DataBase List > Eltrombopag Olamine

Eltrombopag Olamine

Product Name
Eltrombopag Olamine
CAS No.
496775-62-3
Chemical Name
Eltrombopag Olamine
Synonyms
Eltrombopag olamine;Eltrombopag Diolamine;EltroMbopag OlaMine API;Revolade;Sb 497115gr;Unii-4U07F515;ELTROMBOPAG OL;Unii-4U07F515lg;Eltrombopag API;Promacta Olamine
CBNumber
CB82495099
Molecular Formula
C27H29N5O5
Formula Weight
503.56
MOL File
496775-62-3.mol
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Eltrombopag Olamine Property

storage temp. 
under inert gas (nitrogen or Argon) at 2–8 °C
solubility 
DMSO:56.33(Max Conc. mg/mL);99.76(Max Conc. mM)
DMF:1.0(Max Conc. mg/mL);1.77(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.44(Max Conc. mM)
Ethanol:0.1(Max Conc. mg/mL);0.18(Max Conc. mM)
form 
Powder
color 
Purple to black
Stability:
Hygroscopic
InChIKey
LQQUHOUXABUDJA-OUFJFOJPSA-N
SMILES
C(N)CO.O=C1/C(/C(C)=NN1C1C=CC(C)=C(C)C=1)=N\NC1C=CC=C(C2C=CC=C(C(=O)O)C=2)C=1O
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H319Causes serious eye irritation

H412Harmful to aquatic life with long lasting effects

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TRC
Product number
E508100
Product name
EltrombopagOlamine
Packaging
5mg
Price
$65
Updated
2021/12/16
AK Scientific
Product number
3608AH
Product name
Eltrombopagolamine
Packaging
10mg
Price
$75
Updated
2021/12/16
ApexBio Technology
Product number
A3387
Product name
EltrombopagOlamine
Packaging
10mM(in 1mL DMSO)
Price
$90
Updated
2021/12/16
Biosynth Carbosynth
Product number
FD157443
Product name
3'-[(2Z)-2-[1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid compd.with 2-aminoethanol
Packaging
1g
Price
$100
Updated
2021/12/16
ChemScene
Product number
CS-1566
Product name
Eltrombopag(Olamine)
Purity
99.96%
Packaging
10mg
Price
$114
Updated
2021/12/16
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Eltrombopag Olamine Chemical Properties,Usage,Production

Description

Eltrombopag Olamine is used to treat low blood platelet counts in adults with chronic immune (idiopathic) thrombocytopenia (ITP), when certain other medicines, or surgery to remove the spleen, have not worked well enough. It has also been recently approved (late 2012) for the treatment of thrombocytopenia (low blood platelet counts) in patients with chronic hepatitis C.

Uses

Treatment of chemotherapy-induced thrombocytopenia and treatment of immune thrombocytopenic purpura.

Clinical Use

Eltrombopag olamine, a thrombopoietin receptor (TpoR) agonist, was approved in late 2008 for the once-daily, oral short-term and long-term treatment of adult patients with previously treated chronic idiopathic thrombocytopenic purpura (ITP). It is the first small-molecule TpoR agonist and was launched in the U.S. for this indication in 2009 by GlaxoSmithKline (GSK). Because eltrombopag is a small molecule, the drug is administered orally and has a reduced potential for causing an immune system reaction versus alternative protein-based therapies. In 2010, eltrombopag was approved in Europe for the long-term treatment of adult patients with previously treated chronic ITP.

Synthesis

The synthesis began with the nitration of 2-bromophenol (39) with sodium nitrate and sulfuric acid in water at 10??C to give 2-bromo-6-nitrophenol (40) in 25% yield, which was methylated using methyl iodide and potassium carbonate in refluxing acetone providing 2-bromo- 6-nitroanisole (41) in 76% yield (the Scheme).40 Suzuki coupling of compound 41 with 3-carboxyphenyl boronic acid with Pd(PPh3)4 and 2 M sodium carbonate in refluxing dioxane gave 20-methoxy- 30-nitrobiphenyl-3-carboxylic acid (42) in 47% yield as a tan powder. Demethylation using 48% HBr (aq) in refluxing acetic acid resulted in a 79% yield of 20-hydroxy-30-nitrobiphenyl-3-carboxylic acid (43). The nitro group of compound 43 was reduced via catalytic hydrogenation at 50 psi at room temperature over Pd/C in mixed ethanol/3 M aq NaOH solution to give 30-amino-20-hydroxybiphenyl- 3-carboxylic acid (44) in quantitative yield. The intermediate 1-(3,4-dimethylphenyl)-3-methyl-2,5-dihydro-1Hpyrazol- 5-one (47) was prepared by condensing of 3,4-dimethylphenyl- hydrazine 45 with ethyl acetoacetate 46 with sodium acetate in refluxing acetic acid in 76% yield. Treatment of (44) with sodium nitrite in 1 M HCl at 5??C, followed by condensation with 1-(3,4-dimethylphenyl)-3-methyl-2,5-dihydro-1H-pyrazol-5-one (47) at a constant pH of 7¨C8 via the addition of sodium bicarbonate and ethanol afforded eltrombopag in 32% yield. Finally, eltrombopag was treated with hydroxyl ethylamine to give eltrombopag olamine (VIII).

in vivo

Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees[1].
Eltrombopag Olamine (17.6 mg/kg; IP; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection[3].

Animal Model:Female chimpanzees[1]
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once a day; for 5 days
Result:Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.
Animal Model:C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 108 CFU suspended in 40 μL PBS) into the nasal cavities)[3]
Dosage:17.6 mg/kg
Administration:IP; once a day for 2 days
Result:Significantly reduced mean bacterial counts (5.0 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) mice.

Eltrombopag Olamine Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Eltrombopag Olamine manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Eltrombopag olamine 496775-62-3
Price
US $0.00/g
Min. Order
1g
Purity
98.0%min
Supply Ability
10KGS
Release date
2021-06-23
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Eltrombopag olamine 496775-62-3
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
50kg/Month
Release date
2024-07-23
Dingwang Technology (Wuhan) Co., Ltd.
Product
Eltrombopag Olamine 496775-62-3
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
20 TONS
Release date
2022-11-07

496775-62-3, Eltrombopag OlamineRelated Search:


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