avatrombopag

Modify Date: 2024-01-02 19:13:10

avatrombopag structure	Common Name	avatrombopag
	CAS Number	570406-98-3	Molecular Weight	649.655
	Density	1.4±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C29H34Cl2N6O3S2	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Purity		Quantity		Budget		Inquiry

Use of avatrombopag Avatrombopag(AKR-501; AS1670542) is a novel orally-active thrombopoietin(TPO) receptor agonist with EC50 of 3.3 nM.EC50 value: 3.3 nM [1]Target: TPO receptor agonistin 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].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].

• Properties

• Spectrum

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 Names

Name	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
Synonym	More Synonyms

 avatrombopag Biological Activity

Description	Avatrombopag(AKR-501; AS1670542) is a novel orally-active thrombopoietin(TPO) receptor agonist with EC50 of 3.3 nM.EC50 value: 3.3 nM [1]Target: TPO receptor agonistin 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].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].
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> Thrombopoietin Receptor Research Areas >> Inflammation/Immunology
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.

 Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Molecular Formula	C29H34Cl2N6O3S2
Molecular Weight	649.655
Exact Mass	648.151062
PSA	161.87000
LogP	6.82
Index of Refraction	1.671
Storage condition	2-8℃

 Synonyms

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