Hetrombopag

Hetrombopag is an orally active human thrombopoietin receptor agonist. Hetrombopag protects Cardiomyocyte Survival from Oxidative Stress Damage as an Enhancer of Stem Cells. Hetrombopag specifically stimulated proliferation and/or differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells, with low nanomolar EC50 values through stimulation of STAT, PI3K and ERK signalling pathways. Notably, hetrombopag effectively up-regulated G1 -phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalized progression of the cell cycle, and prevented apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells.

Product information

CAS Number: 1257792-41-8

Molecular Weight: 458.47

Formula: C25H22N4O5

Synonym:

SHR8735

SHR 8735

SHR-8735

Chemical Name: (E)-5-(2-hydroxy-3-(2-(3-methyl-5-oxo-1-(5, 6, 7, 8-tetrahydronaphthalen-2-yl)-1, 5-dihydro-4H-pyrazol-4-ylidene)hydrazinyl)phenyl)furan-2-carboxylic acid

Smiles: CC1=NN(C2=CC3CCCCC=3C=C2)C(=O)/C/1=N/NC1=CC=CC(C2=CC=C(O2)C(O)=O)=C1O

InChiKey: BDGGFTDRPHKXFC-HPNDGRJYSA-N

InChi: InChI=1S/C25H22N4O5/c1-14-22(24(31)29(28-14)17-10-9-15-5-2-3-6-16(15)13-17)27-26-19-8-4-7-18(23(19)30)20-11-12-21(34-20)25(32)33/h4,7-13,26,30H,2-3,5-6H2,1H3,(H,32,33)/b27-22+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Xie C, Zhao H, Bao X, Fu H, Lou L. Pharmacological characterization of hetrombopag, a novel orally active human thrombopoietin receptor agonist. J Cell Mol Med. 2018 Nov;22(11):5367-5377. doi: 10.1111/jcmm.13809. Epub 2018 Aug 29. PubMed PMID: 30156363; PubMed Central PMCID: PMC6201220.
2. Zheng L, Liang MZ, Zeng XL, Li CZ, Zhang YF, Chen XY, Zhu X, Xiang AB. Safety, Pharmacokinetics and Pharmacodynamics of Hetrombopag Olamine, a Novel TPO-R Agonist, in Healthy Individuals. Basic Clin Pharmacol Toxicol. 2017 Nov;121(5):414-422. doi: 10.1111/bcpt.12815. Epub 2017 Jun 22. PubMed PMID: 28544774.
3. Zhou N, Wang J, Li X, Zhao Y, Sun Y, Zou C. Hetrombopag, a Thrombopoietin Receptor Agonist, Protects Cardiomyocyte Survival from Oxidative Stress Damage as an Enhancer of Stem Cells. Cardiovasc Drugs Ther. 2016 Dec;30(6):567-577. PubMed PMID: 27838864.
4. Chen T, Chen Z, Zhang S, Zhang K, Wang L. Development and validation of a LC-MS/MS method for quantification of hetrombopag for pharmacokinetics study. Springerplus. 2015 Oct 29;4:652. doi: 10.1186/s40064-015-1446-0. eCollection 2015. PubMed PMID: 26543786; PubMed Central PMCID: PMC4628022.

Products are for research use only. Not for human use.