A thrombopoietin receptor agonist
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Lusutrombopag

Item No. 26533

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-3-[2,6-dichloro-4-[[[4-[3-[(1S)-1-(hexyloxy)ethyl]-2-methoxyphenyl]-2-thiazolyl]amino]carbonyl]phenyl]-2-methyl-2-propenoic acid
CAS Number
1110766-97-6
Molecular Formula
C29H32Cl2N2O5S
Formula Weight
591.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/ml
λmax
218, 260, 322 nm
SMILES
ClC1=C(/C=C(C)/C(O)=O)C(Cl)=CC(C(NC2=NC(C3=CC=CC([C@H](C)OCCCCCC)=C3OC)=CS2)=O)=C1
InChi Code
InChI=1S/C29H32Cl2N2O5S/c1-5-6-7-8-12-38-18(3)20-10-9-11-21(26(20)37-4)25-16-39-29(32-25)33-27(34)19-14-23(30)22(24(31)15-19)13-17(2)28(35)36/h9-11,13-16,18H,5-8,12H2,1-4H3,(H,35,36)(H,32,33,34)/b17-13+/t18-/m0/s1
InChi Key
NOZIJMHMKORZBA-KJCUYJGMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $43

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    5 mg

    $172

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    10 mg

    $280

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    50 mg

    $858

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    Product Description

    Lusutrombopag is an agonist of the thrombopoietin receptor.1 It induces proliferation of Ba/F3 cells expressing human MPL, the gene for the thrombopoietin receptor, with an EC50 value of 84 nM but not of those expressing mouse Mpl.2 Lusutrombopag (0.3-10 mg/kg per day) increases the number of circulating platelets in a transgenic mouse model expressing human MPL and increases the number of megakaryocytes in the bone marrow when administered at a dose of 10 mg/kg per day. Formulations containing lusutrombopag have been used in the treatment of thrombocytopenia in adult patients with chronic liver disease scheduled to undergo invasive procedures.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takayama, M., and Kurose, N. Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity, and intermediate therefor. (2014).

    2. Yoshida, H., Yamada, H., Nogami, W., et al. Development of a new knock-in mouse model and evaluation of pharmacological activities of lusutrombopag, a novel, nonpeptidyl small-molecule agonist of the human thrombopoietin receptor c-Mpl. Exp. Hematol. 59, 30-39 (2018).