ACT-132577 (Synonyms: ACT-132577) |
Catalog No.GC13236
One-Click Copy Product Info
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ACT-132577 (ACT-132577) is the major and pharmacologically active metabolite of Macitentan.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1103522-45-7
Sample solution is provided at 25 µL, 10mM.
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ACT-132577 is a dual antagonist of ETA and ETB receptors with IC50 values of 3.4nM and 987nM, respectively [1].
ACT-132577 is a major metabolite of macitentan which is a dual ET receptor antagonist with strong affinity for the tissues. Macitentan is metabolized into ACT-132577 in vivo. ACT-132577 is also a dual ET receptor antagonist and has a longer half-life than its parent compound. In assays using microsomal membranes of CHO cells overexpressing human ETA and ETB receptors, ACT-132577 shows potent effects on ETA and ETB receptors with IC50 values of 3.4nM and 987nM, respectively. In the in vitro functional assay, ACT-132577 completely inhibits the intracellular calcium increase induced by ET-1with IC50 values of 14nM, 5.8nM and 10.9nM in HPASMC, RASMC and m3T3 cells, respectively. ACT-132577 also causes a significant reduction of sarafotoxin S6c-induced contraction in isolated rat trachea [1].
In normotensive rats, administration of macitentan increases plasma ET-1 concentration. In hypertensive DOCA-salt rats, macitentan decreases mean arterial blood pressure. Besides that, macitentan suppresses the development of pulmonary hypertension and right ventricle hypertrophy in the monocrotaline model of pulmonary hypertension as well as in the streptozotocin model of diabetes [1].
References:
[1] Iglarz M, Binkert C, Morrison K, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. Journal of Pharmacology and Experimental Therapeutics, 2008, 327(3): 736-745.
| Cas No. | 1103522-45-7 | SDF | |
| Synonyms | ACT-132577 | ||
| Canonical SMILES | BrC1=CC=C(C2=C(OCCOC3=NC=C(Br)C=N3)NC=N/C2=N\S(N)(=O)=O)C=C1 | ||
| Formula | C16H14Br2N6O4S | M.Wt | 546.19 |
| Solubility | DMSO : 25 mg/mL (45.77 mM; ultrasonic and warming and heat to 60°C) | 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 | 1.8309 mL | 9.1543 mL | 18.3086 mL |
| 5 mM | 366.2 μL | 1.8309 mL | 3.6617 mL |
| 10 mM | 183.1 μL | 915.4 μL | 1.8309 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 15 reference(s) in Google Scholar.)