Macitentan-d4 (Synonyms: ACT-064992-d4) |
Catalog No.GC45723
One-Click Copy Product Info
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An internal standard for the quantification of macitentan
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1258428-05-5
Sample solution is provided at 25 µL, 10mM.
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Macitentan-d4 is intended for use as an internal standard for the quantification of macitentan by GC- or LC-MS. Macitentan is a dual antagonist of the endothelin (ET) receptors type A and B (IC50s = 0.5 and 391 nM in a radioligand binding assay using recombinant ETA and ETB, respectively).1 Macitentan inhibits intracellular Ca2+ increases induced by the endothelin isoform ET-1 in human pulmonary arterial smooth muscle cells (HPASMCs; IC50 = 0.9 nM), contractions of isolated rat aortic rings (pA2 = 7.6 for ETA), and sarafotoxin S6c-induced contractions of isolated rat tracheal rings (pA2 = 5.9 for ETB). Macitentan increases plasma ET-1 concentrations in normotensive rats and decreases mean arterial blood pressure in hypertensive DOCA-salt rats (ED50 = 1 mg/kg). Oral administration (30 mg/kg per day) prevents development of pulmonary hypertension and right ventricle hypertrophy in a rat model of hypertension induced by monocrotaline . It also decreases the number of vascular and tubule-interstitial lesions and amount of glomerular damage in a rat model of diabetes induced by streptozotocin . Formulations containing macitentan have been used for the treatment of pulmonary arterial hypertension.2
|1. Iglarz, M., Binkert, C., Morrison, K., et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 327(3), 736-745 (2008).|2. Lefaucheur, C., Loupy, A., and Zeevi, A. Complement-binding anti-HLA antibodies and kidney transplantation. N. Engl. J. Med. 370(1), 85-86 (2014).
| Cas No. | 1258428-05-5 | SDF | |
| Synonyms | ACT-064992-d4 | ||
| Canonical SMILES | BrC1=CC=C(C2=C(OC([2H])([2H])C([2H])([2H])OC3=NC=C(Br)C=N3)N=CN=C2NS(NCCC)(=O)=O)C=C1 | ||
| Formula | C19H16Br2D4N6O4S | M.Wt | 592.3 |
| Solubility | DMSO : 100 mg/mL (168.83 mM; ultrasonic and warming and heat to 80°C); DMSO : ≥ 50 mg/mL (84.42 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 | 1.6883 mL | 8.4417 mL | 16.8833 mL |
| 5 mM | 337.7 μL | 1.6883 mL | 3.3767 mL |
| 10 mM | 168.8 μL | 844.2 μL | 1.6883 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)