TD-0212 TFA |
Catalog No.GC38856
One-Click Copy Product Info
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Le TD-0212 TFA est un antagoniste des récepteurs de l'angiotensine II de type 1 (AT1) et un inhibiteur de la néprilysine (NEP) À double pharmacologie active par voie orale, avec un pKi de 8,9 pour AT1 et un pIC50 de 9,2 pour NEP.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1073549-11-7
Sample solution is provided at 25 µL, 10mM.
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TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].
TD-0212 provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition[1].
TD-0212 produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and -independent hypertension[1].
[1]. McKinnell RM, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med Chem Lett. 2018 Dec 3;10(1):86-91.
| Cas No. | 1073549-11-7 | SDF | |
| Canonical SMILES | OC(C(F)(F)F)=O.OC(C1=CC=CC=C1C2=CC=C(CN3C(CNC([C@H](CC(C)C)S)=O)=C(CC)N=C3OCC)C(F)=C2)=O | ||
| Formula | C30H35F4N3O6S | M.Wt | 641.67 |
| Solubility | DMSO: 125 mg/mL (194.80 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5584 mL | 7.7922 mL | 15.5843 mL |
| 5 mM | 311.7 μL | 1.5584 mL | 3.1169 mL |
| 10 mM | 155.8 μL | 779.2 μL | 1.5584 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)