TDI-10229 |
| カタログ番号GC63213 |
TDI-10229 は、可溶性アデニル酸シクラーゼ (sAC、ADCY10) の強力な経口投与可能な阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2810887-45-5
Sample solution is provided at 25 µL, 10mM.
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TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound[1][2].
TDI-10229 exhibits good permeability with an IC50 of 92 nM for human 4-4 cells[2].
TDI-10229 (5 mg/kg; p.o.) treatment shows the Cmax, AUC and MRT were 15.5 μM, 94 μg h/mL and 3.95 hours, respectively.
[1]. Balbach M, et al. Soluble adenylyl cyclase inhibition prevents human sperm functions essential for fertilization [published online ahead of print, 2021 Aug 31]. Mol Hum Reprod. 2021;gaab054.
[2]. Fushimi M, et al. Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10). ACS Med Chem Lett. 2021;12(8):1283-1287. Published 2021 Jul 14.
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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