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Avatrombopag

  Cat. No.:  DC57020   Featured
Chemical Structure
570406-98-3
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Field of application
Avatrombopag, also known as AKR-501, YM477, AS 1670542 or E5501, is a novel orally-active thrombopoietin (TPO) receptor agonist. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501 may be useful in the treatment of patients with thrombocytopenia.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 570406-98-3
Chemical Name: Avatrombopag free base
Synonyms: AKR-501;AS1670542;E5501;UNII-3H8GSZ4SQL;YM477;1-[3-Chloro-5-[[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl]carbamoyl]-2-pyridyl]piperidine-4-carboxylic acid;AKR 501;1-[3-chloro-5-[[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)-1,3-thiazol-2-yl]carbamoyl]pyridin-2-yl]piperidine-4-carboxylic acid;E-5501;4-Piperidinecarboxylic acid, 1-[3-chloro-5-[[[4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl]amino]carbonyl]-2-pyridinyl]-;1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl]carbamoyl}pyridin-2-yl)piperidine-4-carboxylic acid;1-(3-Chloro-5-{[4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-1,3-thiazol-2-yl]carbamoyl}-2-pyridinyl)-4-piperidinecarboxylic acid;1-(3-Chlor-5-{[4-(4-chlor-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-1,3-thiazol-2-yl]carbamoyl}-2-pyridinyl)-4-piperidincarbons�ure [German];Avatrombopag
SMILES: OC(/C=C\C(=O)O)=O.OC(C1CCN(C2N=CC(C(NC3=NC(C4SC=C(Cl)C=4)=C(N4CCN(C5CCCCC5)CC4)S3)=O)=CC=2Cl)CC1)=O
Formula: C29H34Cl2N6O3S2
M.Wt: 649.65
Purity: >98%
Sotrage: 0-4 C for short term (days to weeks), or -20 C for long term (months).
Description: Avatrombopag(AKR-501; AS1670542) is a novel orally-active thrombopoietin(TPO) receptor agonist with EC50 of 3.3 nM.
Target: EC50 value: 3.3 nM [1] TPO receptor agonist
In Vivo: Daily oral administration of AKR-501 dose-dependently increased the number of human platelets in in human platelet producing non-obese diabetic/severe combined immunodeficiency (NOD/SCID) mice transplanted with human fetal liver CD34(+) cells, with significance achieved at doses of 1 mg/kg and above. The peak unbound plasma concentrations of AKR-501 after administration at 1 mg/kg in NOD/SCID mice were similar to those observed following administration of an active oral dose in human subjects [1]. AS1670542 significantly increased the number of human platelets in non-obese diabetic/severe combined immunodeficiency (NOD/SCID) mice with transplanted human hematopoietic stem cells at 0.3 (P<0.05); in contrast, while administration of eltrombopag also increased the numbers of these platelets at 30mg/kg/day (P=0.058), no statistical significance was noted in the increase [2].
In Vitro: AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501, however, was shown to be effective only in humans and chimpanzees with high species specificity [1]. AS1670542 has 50% effective concentration values for cell proliferation with AS1670542 or eltrombopag were 1.9 and 13nM, respectively, while those for megakaryocyte colony formation from human cord blood CD34(+) cells with AS1670542 or eltrombopag were 260 and 950nM, respectively [2].
References: [1]. Fukushima-Shintani M, et al. AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist. Eur J Haematol. 2009 Apr;82(4):247-54. [2]. Abe M, et al. Pharmacological profile of AS1670542, a novel orally-active human thrombopoietin receptor agonist. Eur J Pharmacol. 2011 Jan 10;650(1):58-63.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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