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MedKoo product information:
AKR-501
Description of AKR-501: AKR-501 (YM477) 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. Daily oral administration of
AKR-501
dose-dependently increased the number of human platelets in these mice,
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. These results suggest that
AKR-501 is an
orally-active TPO receptor agonist that may be useful in the treatment
of patients with thrombocytopenia. (source: Eur J Haematol. 2009
Apr;82(4):247-54).
Current developer: AkaRx,
MGI Pharm, Eisai Inc.
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MedKoo Code#:
200127
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Name:
AKR-501
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CAS#:
570406-98-3
Synonym: YM477.
IUPAC/Chemical name:
(1-(3-chloro-5-((4-(4-chloro-2-thienyl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl)carbamoyl)-2-pyridyl)piperidine-4-carboxylic
acid)
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Chemical structure: |
Theoretical analysis
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MedKoo Code#: 200127
Name: AKR-501
CAS#: 570406-98-3
Chemical Formula: C29H34Cl2N6O3S2
Exact Mass: 648.15109
Molecular Weight: 649.65
Elemental Analysis: C, 53.61; H, 5.28; Cl,
10.91; N, 12.94; O, 7.39; S, 9.87
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Availability and price:
AKR-501 is available through custom synthesis.
To inquire the quotation and lead time of custom synthesis for this agent, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Quality control
data:
Product will be shipped with
supporting analytical data.
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Information about this agent
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AKR-501,
a novel, small-molecule thrombopoietin mimetic being investigated for
the treatment of thrombocytopenia. AkaRx is now a wholly-owned
subsidiary of Eisai Inc. and Eisai has the exclusive worldwide rights to
develop, market and manufacture AKR-501. AKR-501 is an investigational
thrombopoietin receptor agonist that, based on preclinical studies,
increases platelet production by stimulating megakaryocytic
proliferation and differentiation. Eisai is currently conducting Phase
II clinical trials of AKR-501 in the United States as a potential
treatment for idiopathic thrombocytopenic purpura (ITP) and
thrombocytopenia associated with liver diseases (TLD), and has confirmed
proof of concept in the clinical studies for ITP. In addition, Eisai
will explore the compound's potential as a treatment for
chemotherapy-induced thrombocytopenia (CIT).
1. Erickson-Miller, Connie L. Non-peptide
thrombopoietin (TPO) receptor agonists for treatment of depression,
fatigue and chronic fatigue syndrome. PCT Int. Appl. (2009), 28pp.
CODEN: PIXXD2 WO 2009151862 A1 20091217
2. Rice, Lawrence. Treatment of immune thrombocytopenic purpura: focus
on eltrombopag. Biologics: Targets & Therapy (2009), 3 151-157.
3. Fukushima-Shintani, Mari; Suzuki, Ken-ichi; Iwatsuki, Yoshiyuki; Abe,
Masaki; Sugasawa, Keizo; Hirayama, Fukushi; Kawasaki, Tomihisa; Nakahata,
Tatsutoshi. AKR-501 (YM477) a novel orally-active thrombopoietin
receptor agonist. European Journal of Haematology (2009), 82(4),
247-254.
4. Vadhan-Raj, Saroj. Management of chemotherapy-induced
thrombocytopenia: current status of thrombopoietic agents. Seminars in
Hematology (2009), 46(1, Suppl. 2), S26-S32. CODEN: SEHEA3
ISSN:0037-1963. CAN 151:259412 AN 2009:415206
5. Fukushima-Shintani, Mari; Suzuki, Ken-ichi; Iwatsuki, Yoshiyuki; Abe,
Masaki; Sugasawa, Keizo; Hirayama, Fukushi; Kawasaki, Tomihisa. AKR-501
(YM477) in combination with thrombopoietin enhances human
megakaryocytopoiesis. Experimental Hematology (New York, NY, United
States) (2008), 36(10), 1337-1342.
6. Peeters, Karen; Stassen, Jean-Marie; Collen, Desire; Van Geet, Chris;
Freson, Kathleen. Emerging treatments for thrombocytopenia: Increasing
platelet production. Drug Discovery Today (2008), 13(17/18), 798-806.
7. Erickson-Miller, Connie Lynn. Thrombopoietin receptor agonist for
treatment of cancer. PCT Int. Appl. (2008), 53 pp. CODEN: PIXXD2 WO
2008101141 A2 20080821 CAN 149:282993 AN 2008:1008939
8. Erickson-Miller, Connie L.; Jenkins, Julian; Theodore, Dickens. TPO
receptor agonist combination with other antiviral therapy for the
treatment of viral diseases. PCT Int. Appl. (2008), 50pp. CODEN: PIXXD2
WO 2008073864 A1 20080619 CAN 149:45179 AN 2008:735884
9. Desjardins, Robert E.; Lucek, Rudolph. Compositions containing a
small molecule c-Mpl agonist that mimics thrombopoietin and methods for
increasing blood platelet levels in humans. U.S. Pat. Appl. Publ.
(2008), 14pp. CODEN: USXXCO US 2008039475 A1 20080214
10. Suzuki, Ken-Ichi; Sugasawa, Keizo. Compositions and methods for
treating thrombocytopenia. PCT Int. Appl. (2007), 47pp. CODEN: PIXXD2 WO
2007054783 A2 20070518 CAN 146:528295 AN 2007:538881
11. Sugasawa, Keizo; Watanuki, Susumu; Koga, Yuji; Nagata, Hiroshi;
Obitsu, Kazuyoshi; Wakayama, Ryutaro; Hirayama, Fukushi; Suzuki, Ken-ichi.
Preparation of 2-acylaminothiazole derivatives or salts thereof as c-Mpl
receptor ligands. PCT Int. Appl. (2003), 110 pp. CODEN: PIXXD2 WO
2003062233 A1 20030731
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