Synonym
Tavapadon; PF-6649751; PF 6649751; PF6649751; CVL-751; CVL 751; CVL751;
IUPAC/Chemical Name
1,5-dimethyl-6-[2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]oxyphenyl]pyrimidine-2,4-dione
InChi Key
AKQXQLUNFKDZBN-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H16F3N3O3/c1-10-9-12(28-17-14(19(20,21)22)5-4-8-23-17)6-7-13(10)15-11(2)16(26)24-18(27)25(15)3/h4-9H,1-3H3,(H,24,26,27)
SMILES Code
O=C1NC(C(C)=C(C2=CC=C(OC3=NC=CC=C3C(F)(F)F)C=C2C)N1C)=O
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
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
391.35
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.
| 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: Kumar S, Rastogi SK, Roy S, Sharma K, Kumar S, Maity D, Chand D, Vishwakarma S, Gayen JR, Srivastava KR, Kumar R, Yadav PN. Discovery and structure - activity relationships of 2,4,5-trimethoxyphenyl pyrimidine derivatives as selective D5 receptor partial agonists. Bioorg Chem. 2024 Sep 7;153:107809. doi: 10.1016/j.bioorg.2024.107809. Epub ahead of print. PMID: 39270528.
2: Lewis MM, Van Scoy LJ, De Jesus S, Hakun JG, Eslinger PJ, Fernandez-Mendoza J, Kong L, Yang Y, Snyder BL, Loktionova N, Duvvuri S, Gray DL, Huang X, Mailman RB. Dopamine D1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease. Biomolecules. 2023 May 12;13(5):829. doi: 10.3390/biom13050829. PMID: 37238699; PMCID: PMC10216182.
3: Bezard E, Gray D, Kozak R, Leoni M, Combs C, Duvvuri S. Rationale and Development of Tavapadon, a D1/D5-Selective Partial Dopamine Agonist for the Treatment of Parkinson's Disease. CNS Neurol Disord Drug Targets. 2024;23(4):476-487. doi: 10.2174/1871527322666230331121028. PMID: 36999711; PMCID: PMC10909821.
4: Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S. Ligand recognition and biased agonism of the D1 dopamine receptor. Nat Commun. 2022 Jun 8;13(1):3186. doi: 10.1038/s41467-022-30929-w. PMID: 35676276; PMCID: PMC9177848.
