[CAS NO. 2810887-45-5] TDI-10229
PRODUCTS SPECIFICATIONS [2810887-45-5]
DESCRIPTION [2810887-45-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 313.78 |
| Molecular Formula | C16H16ClN5 |
| SMILES | NC1=NC(C2=NN(C)C(C)=C2CC3=CC=CC=C3)=CC(Cl)=N1 |
Summary
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 ( IC 50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound [1] [2] .
IC50 & Target
IC 50 : 195 nM (sAC) [2] .
In Vitro
TDI-10229 exhibits good permeability with an IC 50 of 92 nM for human 4-4 cells [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TDI-10229 (5 mg/kg; p.o.) treatment shows the C
max
, AUC and MRT were 15.5 μM, 94 μg h/mL and 3.95 hours, respectively.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Mouse [2] |
| Dosage: | 20 mg/kg |
| Administration: | P.o.(Pharmacokinetic Analysis) |
| Result: | The C max , AUC and MRT were 15.5 μM, 94 μg h/mL and 3.95 hours, respectively. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 398.37 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1869 mL | 15.9347 mL | 31.8695 mL |
| 5 mM | 0.6374 mL | 3.1869 mL | 6.3739 mL |
| 10 mM | 0.3187 mL | 1.5935 mL | 3.1869 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution
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.
- [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.