MedKoo Cat#: 573466 | Name: Mitapivat HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Mitapivat, also known as AG348, is a potent, selective allosteric activator of the enzyme pyruvate kinase (PK), specifically the red blood cell isoform PKR. By enhancing PKR activity, Mitapivat increases glycolytic flux, leading to improved ATP production and redox balance, which is particularly beneficial in conditions such as pyruvate kinase deficiency (PKD) and other hemolytic anemias.Mitapivat directly binds to PKR, increasing its enzymatic activity in purified enzyme systems and red blood cell lysates. It enhances the enzyme's affinity for PEP, boosting its catalytic efficiency. Treatment with Mitapivat in vitro leads to reductions in markers of oxidative stress in red blood cells.

Chemical Structure

Mitapivat HCl
Mitapivat HCl
CAS#2559738-69-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 573466

Name: Mitapivat HCl

CAS#: 2559738-69-9 (HCl)

Chemical Formula: C24H27ClN4O3S

Exact Mass: 486.1492

Molecular Weight: 0.00

Elemental Analysis: C, 59.19; H, 5.59; Cl, 7.28; N, 11.50; O, 9.86; S, 6.58

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1260075-17-9 (free base) 2559738-69-9 (HCl) 2329710-91-8 (sulfate) 2559738-74-6 (tosylate) 2151847-10-6 (sulfate hydrate)
Synonym
Mitapivat HCl; Mitapivat hydrochloride, AG348; AG-348; AG 348;
IUPAC/Chemical Name
N-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide hydrochloride
InChi Key
YONQEXWSPOESJA-UHFFFAOYSA-N
InChi Code
O=S(C1=C2N=CC=CC2=CC=C1)(NC3=CC=C(C(N4CCN(CC5CC5)CC4)=O)C=C3)=O.[H]Cl
SMILES Code
O=S(C1=C2N=CC=CC2=CC=C1)(NC3=CC=C(C(N4CCN(CC5CC5)CC4)=O)C=C3)=O.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 0.00 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Yang H, Merica E, Chen Y, Cohen M, Goldwater R, Kosinski PA, Kung C, Yuan ZJ, Silverman L, Goldwasser M, Silver BA, Agresta S, Barbier AJ. Phase 1 Single- and Multiple-Ascending-Dose Randomized Studies of the Safety, Pharmacokinetics, and Pharmacodynamics of AG-348, a First-in-Class Allosteric Activator of Pyruvate Kinase R, in Healthy Volunteers. Clin Pharmacol Drug Dev. 2019 Feb;8(2):246-259. doi: 10.1002/cpdd.604. Epub 2018 Aug 9. PubMed PMID: 30091852. 2: Kung C, Hixon J, Kosinski PA, Cianchetta G, Histen G, Chen Y, Hill C, Gross S, Si Y, Johnson K, DeLaBarre B, Luo Z, Gu Z, Yao G, Tang H, Fang C, Xu Y, Lv X, Biller S, Su SM, Yang H, Popovici-Muller J, Salituro F, Silverman L, Dang L. AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency. Blood. 2017 Sep 14;130(11):1347-1356. doi: 10.1182/blood-2016-11-753525. Epub 2017 Jul 31. PubMed PMID: 28760888; PubMed Central PMCID: PMC5609468. 3: Christensen RD, Yaish HM, Nussenzveig RH, Agarwal AM. Siblings with severe pyruvate kinase deficiency and a complex genotype. Am J Med Genet A. 2016 Sep;170(9):2449-52. doi: 10.1002/ajmg.a.37828. Epub 2016 Jun 29. PubMed PMID: 27354418. 4: Croasdell G. European Hematology Association - 20th Annual Congress (June 11-14, 2015 - Vienna, Austria). Drugs Today (Barc). 2015 Jul;51(7):441-5. doi: 10.1358/dot.2015.51.7.2375757. PubMed PMID: 26261846.