Eltrombopag olamine|c-mpl agonist|DC Chemicals

Cas No.:	496775-62-3
Chemical Name:	Eltrombopag olamine;Sb 497115gr;Unii-4U07F515lg
Synonyms:	2-aminoethanol,3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid;EltroMbopag;Eltrombopag Diolamine;Eltrombopag olamine;Revolade;(1,1'-Biphenyl)-3-carboxylic acid, 3'-((2Z)-(1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene)hydrazino)-2'-hydroxy-, compound with 2-aminoethanol (1:2);3'-((2Z)-2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)diazanyl)-2'-hydroxybiphenyl-3-carboxylic acid compound with 2-aminoethanol (1:2);Eltrombopag diethanolamine salt;Eltrombopag Olamine [USAN];Promacta;Sb 497115gr;SB-497115GR;SB-497115-GR;Unii-4U07F515lg;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;Eltrombopag olamine;Sb 497115gr;Unii-4U07F515lg;Eltrombopag (Olamine)
SMILES:	O=C(C1=CC(C2=CC=CC(N/N=C3C(C)=NN(C4=CC=C(C)C(C)=C4)C/3=O)=C2O)=CC=C1)O.NCCO.NCCO
Formula:	C₂₅H₂₂N₄O₄^.₂(C₂H₇NO)
M.Wt:	564.6394
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis. IC50 Value: 0.27 uM (EC50 in murine BAF3 cells) Potential advantages of eltrombopag may include a sustained platelet response and a good tolerability profile. in vitro: Eltrombopag demonstrated a half maximal effective concentration (EC50) of 0.27 uM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR) . Eltrombopag stimulates the growth of TPO-dependent cell lines via JAK2 and STAT signaling pathways and stimulates isolated human CD34+ cells to become megakaryocytes and produce platelets. in vivo: Twelve weeks of antiviral therapy, with concurrent receipt of eltrombopag or placebo, were completed by 36%, 53%, and 65% of patients receiving 30 mg, 50 mg, and 75 mg of eltrombopag, respectively, and by 6% of patients in the placebo group . Eltrombopag was administered as once-daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50, and 75 mg. The pharmacokinetics of eltrombopag was dose dependent and linear, and eltrombopag increased platelet counts in a dose-dependent manner. Toxicity: There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication . Long-term treatment with eltrombopag was generally safe, well tolerated, and effective in maintaining platelet counts in the desired range. Clinical trial: Eltrombopag In Cord Blood Or Haploidentical Bone Marrow Transplantation. For the detailed information of Eltrombopag olamine, the solubility of Eltrombopag olamine in water, the solubility of Eltrombopag olamine in DMSO, the solubility of Eltrombopag olamine in PBS buffer, the animal experiment (test) of Eltrombopag olamine, the cell expriment (test) of Eltrombopag olamine, the in vivo, in vitro and clinical trial test of Eltrombopag olamine, the EC50, IC50,and affinity,of Eltrombopag olamine, For the detailed information of Eltrombopag olamine, the solubility of Eltrombopag olamine in water, the solubility of Eltrombopag olamine in DMSO, the solubility of Eltrombopag olamine in PBS buffer, the animal experiment (test) of Eltrombopag olamine, the cell expriment (test) of Eltrombopag olamine, the in vivo, in vitro and clinical trial test of Eltrombopag olamine, the EC50, IC50,and affinity,of Eltrombopag olamine, Please contact DC Chemicals.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.
DC75816	Nisoxetine	Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.
DC75202	Fosaprepitant free acid	Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4
DC74684	ZH8667	ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.
DC74646	EB-PSMA-617	EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.
DC74641	HC-258	HC-258 is a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. Co-crystallization with hTEAD2 confirmed that HC-258 binds within TEAD’s PA pocket, where it forms a covalent bond with its cysteine.
DC74639	Oligopeptide-10	Oligopeptide-10, also known as granactive oligopeptide-10, is a synthetic bio-active peptide composed of 15 amino acids. it can help manage acne-causing bacteria, both on its own and in conjunction with anti-acne superstar exfoliant salicylic acid.
DC74638	GLPG3667	GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation.