TDI-10229
Based on 1 Customer Validation
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.
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- Purity: 99.00%
- CAS No.: 2810887-45-5
- 화학식: C16H16ClN5
- 분자량:313.78
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
IC50: 195 nM (sAC)[2].
TDI-10229 exhibits good permeability with an IC50 of 92 nM for human 4-4 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse[2]
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Dosage:20 mg/kg
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Administration:P.o.(Pharmacokinetic Analysis)
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Result:The Cmax, AUC and MRT were 15.5 μM, 94 μg h/mL and 3.95 hours, respectively.
Chemical Information
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CAS No. 2810887-45-5
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Appearance Solid
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분자량 313.78
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화학식 C16H16ClN5
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Color White to off-white
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SMILES
CC1=C(C(C2=CC(Cl)=NC(N)=N2)=NN1C)CC3=CC=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 125 mg/mL (398.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1869 mL | 15.9347 mL | 31.8695 mL | 79.6737 mL |
| 5 mM | 0.6374 mL | 3.1869 mL | 6.3739 mL | 15.9347 mL | |
| 10 mM | 0.3187 mL | 1.5935 mL | 3.1869 mL | 7.9674 mL | |
| 15 mM | 0.2125 mL | 1.0623 mL | 2.1246 mL | 5.3116 mL | |
| 20 mM | 0.1593 mL | 0.7967 mL | 1.5935 mL | 3.9837 mL | |
| 25 mM | 0.1275 mL | 0.6374 mL | 1.2748 mL | 3.1869 mL | |
| 30 mM | 0.1062 mL | 0.5312 mL | 1.0623 mL | 2.6558 mL | |
| 40 mM | 0.0797 mL | 0.3984 mL | 0.7967 mL | 1.9918 mL | |
| 50 mM | 0.0637 mL | 0.3187 mL | 0.6374 mL | 1.5935 mL | |
| 60 mM | 0.0531 mL | 0.2656 mL | 0.5312 mL | 1.3279 mL | |
| 80 mM | 0.0398 mL | 0.1992 mL | 0.3984 mL | 0.9959 mL | |
| 100 mM | 0.0319 mL | 0.1593 mL | 0.3187 mL | 0.7967 mL |
TDI-10229 Related Classifications
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