TDI-10229

For research use only. Not for therapeutic Use.

  • CAT Number: I045386
  • CAS Number: 2810887-45-5
  • Molecular Formula: C16H16ClN5
  • Molecular Weight: 313.78
  • Purity: ≥95%
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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.


CAS Number 2810887-45-5
Synonyms

4-(4-benzyl-1,5-dimethylpyrazol-3-yl)-6-chloropyrimidin-2-amine

Molecular Formula C16H16ClN5
Purity ≥95%
InChI InChI=1S/C16H16ClN5/c1-10-12(8-11-6-4-3-5-7-11)15(21-22(10)2)13-9-14(17)20-16(18)19-13/h3-7,9H,8H2,1-2H3,(H2,18,19,20)
InChIKey VSMTYSWGHKYXOF-UHFFFAOYSA-N
SMILES CC1=C(C(=NN1C)C2=CC(=NC(=N2)N)Cl)CC3=CC=CC=C3
Reference

[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.
 [Content Brief]

[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.
 [Content Brief]

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