Mitapivat - 98%, high purity , Pyruvate kinase isozymes R/L activator, CAS No.1260075-17-9, Pyruvate kinase isozymes R/L activator

Item Number
M413491
Grouped product items
SKUSizeAvailabilityPrice Qty
M413491-5mg
5mg
In stock
$98.90
M413491-25mg
25mg
In stock
$445.90
M413491-50mg
50mg
In stock
$474.90
M413491-100mg
100mg
In stock
$771.90

PKM Activators

Basic Description

SynonymsNSC57807 | mitapivatum | n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide | compound 80a (WO2011002817A1) | Red Cell Pyruvate Kinase Activator AG-348 | PKR-IN-1; PKM2 activator 1020; PKM2 activator;AG348;AG-348;AG 348 | BCP1
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsMitapivat (AG-348) is an activator of a pyruvate kinase PKM2, an enzyme involved in glycolysis.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeACTIVATOR, ALLOSTERIC MODULATOR
Mechanism of actionPyruvate kinase isozymes R/L activator
Product Description

Information

Mitapivat Mitapivat (AG-348) is an activator of a pyruvate kinase PKM2 , an enzyme involved in glycolysis.

Product Properties

ALogP2.695
HBD Count1
Rotatable Bond6

Associated Targets(Human)

PKM Tchem Pyruvate kinase PKM (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PKLR Tclin Pyruvate kinase PKLR (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Associated Targets(non-human)

Pkm Pyruvate kinase isozymes M1/M2 (66 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[4-[4-(cyclopropylmethyl)piperazine-1-carbonyl]phenyl]quinoline-8-sulfonamide
INCHI InChI=1S/C24H26N4O3S/c29-24(28-15-13-27(14-16-28)17-18-6-7-18)20-8-10-21(11-9-20)26-32(30,31)22-5-1-3-19-4-2-12-25-23(19)22/h1-5,8-12,18,26H,6-7,13-17H2
InChi Key XAYGBKHKBBXDAK-UHFFFAOYSA-N
Canonical SMILES C1CC1CN2CCN(CC2)C(=O)C3=CC=C(C=C3)NS(=O)(=O)C4=CC=CC5=C4N=CC=C5
Isomeric SMILES C1CC1CN2CCN(CC2)C(=O)C3=CC=C(C=C3)NS(=O)(=O)C4=CC=CC5=C4N=CC=C5
PubChem CID 59634741
Molecular Weight 450.55

Certificates

Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
I2224535Certificate of AnalysisMay 31, 2022 M413491
I2224536Certificate of AnalysisMay 31, 2022 M413491
I2224563Certificate of AnalysisMay 31, 2022 M413491
I2224565Certificate of AnalysisMay 31, 2022 M413491

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 45 mg/mL (99.87 mM); Ethanol: 2 mg/mL (4.43 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility90
DMSO(mM) Max Solubility199.755853956276
Water(mg / mL) Max Solubility<1

Related Documents

References

1. Canu G, De Bonis M, Minucci A, Capoluongo E.  (2016)  Red blood cell PK deficiency: An update of PK-LR gene mutation database..  Blood Cells Mol Dis,  57  (13): (100-9).  [PMID:26832193] [10.1021/op500134e]
2. Kung C, Hixon J, Kosinski PA, Cianchetta G, Histen G, Chen Y, Hill C, Gross S, Si Y, Johnson K et al..  (2017)  AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency..  Blood,  130  (11): (1347-1356).  [PMID:28760888] [10.1021/op500134e]
3. Grace RF, Rose C, Layton DM, Galactéros F, Barcellini W, Morton DH, van Beers EJ, Yaish H, Ravindranath Y, Kuo KHM et al..  (2019)  Safety and Efficacy of Mitapivat in Pyruvate Kinase Deficiency..  N Engl J Med,  381  (10): (933-944).  [PMID:31483964] [10.1021/op500134e]
4. Al-Samkari H, Galactéros F, Glenthøj A, Rothman JA, Andres O, Grace RF, Morado-Arias M, Layton DM, Onodera K, Verhovsek M et al..  (2022)  Mitapivat versus Placebo for Pyruvate Kinase Deficiency..  N Engl J Med,  386  (15): (1432-1442).  [PMID:35417638] [10.1021/op500134e]
5. Rab MAE, Van Oirschot BA, Kosinski PA, Hixon J, Johnson K, Chubukov V, Dang L, Pasterkamp G, Van Straaten S, Van Solinge WW et al..  (2021)  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,  106  (1): (238-249).  [PMID:31974203] [10.1021/op500134e]

Solution Calculators