Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | 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
Synonyms | NSC57807 | 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 & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Mitapivat (AG-348) is an activator of a pyruvate kinase PKM2, an enzyme involved in glycolysis. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ACTIVATOR, ALLOSTERIC MODULATOR |
Mechanism of action | Pyruvate 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. |
ALogP | 2.695 |
---|---|
HBD Count | 1 |
Rotatable Bond | 6 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
---|
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 |
PubChem CID | 59634741 |
---|---|
CAS Registry No. | 1260075-17-9 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
I2224535 | Certificate of Analysis | May 31, 2022 | M413491 |
I2224536 | Certificate of Analysis | May 31, 2022 | M413491 |
I2224563 | Certificate of Analysis | May 31, 2022 | M413491 |
I2224565 | Certificate of Analysis | May 31, 2022 | M413491 |
Solubility | Solubility (25°C) In vitro DMSO: 45 mg/mL (99.87 mM); Ethanol: 2 mg/mL (4.43 mM); Water: Insoluble; |
---|---|
DMSO(mg / mL) Max Solubility | 90 |
DMSO(mM) Max Solubility | 199.755853956276 |
Water(mg / mL) Max Solubility | <1 |
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] |