Synonym
MK-7145; MK 7145; MK7145.
IUPAC/Chemical Name
5,5'-((1R,1'R)-piperazine-1,4-diylbis(1-hydroxyethane-2,1-diyl))bis(4-methylisobenzofuran-1(3H)-one)
InChi Key
OCKGFTQIICXDQW-ZEQRLZLVSA-N
InChi Code
InChI=1S/C26H30N2O6/c1-15-17(3-5-19-21(15)13-33-25(19)31)23(29)11-27-7-9-28(10-8-27)12-24(30)18-4-6-20-22(16(18)2)14-34-26(20)32/h3-6,23-24,29-30H,7-14H2,1-2H3/t23-,24-/m0/s1
SMILES Code
O[C@H](C1=CC=C(C(OC2)=O)C2=C1C)CN3CCN(C[C@H](O)C4=CC=C(C(OC5)=O)C5=C4C)CC3
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, not in water
Shelf Life
>2 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
ROMK, the renal outer medullary potassium channel, is involved in potassium recycling at the thick ascending loop of Henle and potassium secretion at the cortical collecting duct in the kidney nephron. Because of this dual site of action, selective inhibitors of ROMK are expected to represent a new class of diuretics/natriuretics with superior efficacy and reduced urinary loss of potassium compared to standard-of-care loop and thiazide diuretics.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
466.53
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 |
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure
Haifeng Tang, Yuping Zhu, Nardos Teumelsan, Shawn P. Walsh, Aurash Shahripour, Birgit T. Priest, Andrew M. Swensen, John P. Felix, Richard M. Brochu, Timothy Bailey, Brande Thomas-Fowlkes, Lee-Yuh Pai, Caryn Hampton, Aaron Corona, Melba Hernandez, Joseph Metzger, Michael Forrest, Xiaoyan Zhou, Karen Owens, Vincent Tong, Emma Parmee, Sophie Roy, Gregory J. Kaczorowski, Lihu Yang, Magdalena Alonso-Galicia, Maria L. Garcia, and Alexander Pasternak
Publication Date (Web): May 12, 2016 (Letter)
DOI: 10.1021/acsmedchemlett.6b00122
