Tebapivat (PKR activator 2) is a potent activator of pyruvate kinase R (PKR). For more details, check and find compound 385 from the patent WO2019035863A1. Yes Yes

Physicochemical Properties

Molecular Formula	C18H16N8OS
Molecular Weight	392.44
Exact Mass	392.116
CAS #	2283422-04-6
PubChem CID	137501615
Appearance	White to off-white solid powder
LogP	1.2
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	4
Heavy Atom Count	28
Complexity	635
Defined Atom Stereocenter Count	0
SMILES	C1=CC=C(N=C1N)CN1C(=O)C2N(C)C3N=C(CC4C=CNN=4)SC=3C=2C=N1
InChi Key	DIUOELXIXSCFCR-UHFFFAOYSA-N
InChi Code	InChI=1S/C18H16N8OS/c1-25-15-12(16-17(25)23-14(28-16)7-10-5-6-20-24-10)8-21-26(18(15)27)9-11-3-2-4-13(19)22-11/h2-6,8H,7,9H2,1H3,(H2,19,22)(H,20,24)
Chemical Name	10-[(6-aminopyridin-2-yl)methyl]-7-methyl-4-(1H-pyrazol-5-ylmethyl)-3-thia-5,7,10,11-tetrazatricyclo[6.4.0.02,6]dodeca-1(8),2(6),4,11-tetraen-9-one
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Tebapivat (Compound 385) activates wild-type PKR, PKR K410E, or PKR 510Q when the AC50 is less than 0.3 μM [1]. An autosomal recessive mutation in the PKLR gene results in a deficiency of the pyruvate kinase R (PKR) enzyme, which causes pyruvate kinase deficiency (PKD), a condition affecting red blood cells. The following conditions and disorders may benefit from the use of PKR activators: PKD, thalassemia, hereditary elliptocytosis, anemia (e.g., congenital anemia (e.g., enzymopathy)), hemolytic anemia (e.g., hereditary and/or congenital hemolytic anemia, acquired hemolytic anemia), chronic hemolytic anemia caused by phosphoglycerate kinase deficiency, anemia of chronic disease, non-spherocytic hemolytic anemia or hereditary spherocytosis) [1].
References	[1]. Pyruvate kinase activators for use in treating blood disorders. WO2019035863A1.
Additional Infomation	Pyruvate Kinase Activator is any agent that activates the enzyme pyruvate kinase.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~127.41 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 5 mg/mL (12.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.5482 mL	12.7408 mL	25.4816 mL
	5 mM	0.5096 mL	2.5482 mL	5.0963 mL
	10 mM	0.2548 mL	1.2741 mL	2.5482 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.