| CAS NO: | 1260075-17-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 450.56 |
|---|---|
| Formula | C24H26N4O3S |
| CAS No. | 1260075-17-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO:>10 mM |
| Water: NA | |
| Ethanol: NA | |
| Chemical Name | N-{4-[4-(cyclopropylmethyl)piperazine-1-carbonyl]phenyl}quinoline-8-sulfonamide |
| Synonyms | PKM2 activator 1020; AG348; PKM2 activator; PKR-IN-1; AG-348; PKR-IN-1; trade name Pyrukynd |
| SMILES Code | O=S(C1=C2N=CC=CC2=CC=C1)(NC3=CC=C(C(N4CCN(CC5CC5)CC4)=O)C=C3)=O |
| In Vitro | In vitro activity: Mitapivat, previously also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) that has potential use for the treatment of pyruvate kinase deficiency. Mitapivat is a potent human R-type pyruvate kinase (PKR) inhibitor that also shows potency for mutant PKR including R510Q PKR, R532W PKR, T384W PKR etc. Pyruvate kinase type M2, which is expressed in multiple tumor cell types and plays a key role in aerobic glycolysis, has nonglycolytic functions and can regulate transcription and cell proliferation. Thus it has been reported that small molecule activators of pyruvate kinase isozyme M2 (PKM2) may suppress tumor formation but have an unknown effect on established tumors. Cell Assay: Mitapivat (0.1 nM-100 μM; 16 h) activates WT PK-R in RBCs from healthy donors. Mitapivat (0.01 nM-10 μM; 16 h) promotes production of ATP in RBC cells in a dose-dependent manner[1]. |
|---|---|
| In Vivo | Mitapivat (50 mg/kg; p.o.; twice daily for 21 days) improves anemia in a mouse model for β-thalassemia |
| Animal model | WT C57B6 and Hbbth3/+ mice (both are 2-month-old female mice; β-thalassemia model) |
| Formulation & Dosage | 50 mg/kg; In animal feedings; single daily for 3 weeks. |
| References | [1]. Kung C, et al. AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency. Blood. 2017 Sep 14;130(11):1347-1356. [2]. Matte A, et al. The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a β-thalassemia mouse model. J Clin Invest. 2021 May 17;131(10):e144206. [3]. Rab MAE, et al. AG-348 (Mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes. Haematologica. 2021 Jan 1;106(1):238-249. |
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