| Identification | Back Directory | [Name]
TDI-10229 | [CAS]
2810887-45-5 | [Synonyms]
TDI-10229
CompoundTDI10229
TDI 10229,TDI10229
4-(4-benzyl-1,5-dimethyl-1H-pyrazol-3-yl)-6-chloropyrimidin-2-amine
2-Pyrimidinamine, 4-chloro-6-[1,5-dimethyl-4-(phenylmethyl)-1H-pyrazol-3-yl]- | [Molecular Formula]
C16H16ClN5 | [MOL File]
2810887-45-5.mol | [Molecular Weight]
313.78 |
| Chemical Properties | Back Directory | [Boiling point ]
545.3±60.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [solubility ]
DMF: 5 mg/ml
DMSO: 1 mg/ml | [form ]
Solid | [pka]
2.09±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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.
| Animal Model: | Mouse[2] | | Dosage: | 20 mg/kg | | Administration: | P.o.(Pharmacokinetic Analysis) | | Result: | The Cmax, AUC and MRT were 15.5 μM, 94 μg h/mL and 3.95 hours, respectively.
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| [References]
[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. DOI:10.1093/molehr/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. DOI:10.1021/acsmedchemlett.1c00273 |
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