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Macitentan n-butyl analogue, an n-butyl derivative of Macitentan, is an ETA/ETB endothelin (ET) receptor dual antagonist that has potential usefulness in the treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
| ln Vitro |
Risperidone has a Kis of 4.8 and 5.9 nM for the 5-HT2A and D2 dopamine receptors, respectively, making it a strong antagonist of the dopamine receptor, a P-Glycoprotein inhibitor, and a blocker of the serotonin 5-HT2 receptor. In contrast to its dose-dependent induction of IL-10 production, risperidone inhibited the release of IL-12 in mature DCs. Maturated DCs may release TNF-α when given a high dose of risperidone[3].
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| ln Vivo |
In the first experiment, the body weight of the rats treated with risperidone was found to be progressively but slightly lower as a function of age. In the second locomotor experiment, age-dependent variations in body weight are also noted among the three treatment groups. On postnatal days 35, 38, and 41, rats given a 3.0 mg/kg dose of risperidone weighed less than rats given a vehicle treatment. Unlike the smaller, single-sex litters used in the first two locomotor experiments, larger, mixed-sex litters are used in the third experiment. In the third experiment, rats treated with risperidone gained less weight in an age-dependent manner, as was observed in the previous two[4].
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| Animal Protocol |
Rats: There are 211 Long-Evans rats in total—156 males and 56 females. In every study, injections of 1.0 mg/kg of risperidone, 3.0 mg/kg of risperidone, or the vehicle used to deliver the risperidone solution as a control are given to three groups of approximately equal numbers of rats. In the first experiment, twenty-six male rats are tested for locomotor activity for twenty minutes per day starting at postnatal day 49 and continuing daily until postnatal day 53 (n = 9 in the vehicle and 3.0 mg/kg Risperidone group; n = 8 in the 1.0 mg/kg Risperidone group). An additional study examined whether the effects of early-life Risperidone treatment on locomotion continued into adulthood. In a third experiment, the effects of sex on early-life Risperidone's locomotor effects in young adult rats are investigated. Sixty male (n = 20 per treatment group) and fifty-six female (n = 19 rats in the vehicle and 3.0 mg/kg dose group, n = 18 in the 1.0 mg/kg dose group) rats are treated in this experiment. In a fourth experiment, rats given risperidone early in life were evaluated for reversal learning during adulthood. Treatment is given to 42 male rats (n=14 per treatment group)[4].
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| References |
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| Molecular Formula |
C20H21BR2N5O4S
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|---|---|
| Molecular Weight |
587.2848
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| Exact Mass |
586.97
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| CAS # |
556797-16-1
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| Related CAS # |
Macitentan; 441798-33-0
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| Appearance |
Powder
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| SMILES |
CCCCS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br
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| InChi Key |
OZBDTKLWBSATSN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21Br2N5O4S/c1-2-3-10-32(28,29)27-18-17(14-4-6-15(21)7-5-14)19(26-13-25-18)30-8-9-31-20-23-11-16(22)12-24-20/h4-7,11-13H,2-3,8-10H2,1H3,(H,25,26,27)
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| Chemical Name |
N-[5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]pyrimidin-4-yl]butane-1-sulfonamide
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| Synonyms |
Macitentan n-butyl analogue
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7028 mL | 8.5138 mL | 17.0277 mL | |
| 5 mM | 0.3406 mL | 1.7028 mL | 3.4055 mL | |
| 10 mM | 0.1703 mL | 0.8514 mL | 1.7028 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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