CAS 570406-98-3|avatrombopag

Introduction：Basic information about CAS 570406-98-3|avatrombopag, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. avatrombopag BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

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

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 BiologicalActivity

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 ReceptorResearch 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.

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 ReceptorResearch 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
InChIKey	OFZJKCQENFPZBH-UHFFFAOYSA-N
SMILES	O=C(Nc1nc(-c2cc(Cl)cs2)c(N2CCN(C3CCCCC3)CC2)s1)c1cnc(N2CCC(C(=O)O)CC2)c(Cl)c1
Storage condition	2-8℃

Synonyms

avatrombopag

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

E-5501

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

ym477

unii-3h8gsz4sql

4-Piperidinecarboxylic acid, 1-[3-chloro-5-[[[4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl]amino]carbonyl]-2-pyridinyl]-

e5501

akr-501

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