| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
RS-127445 (RS 127445; RS127445) is a novel, potent, selective, and orally bioavailable 5-HT2B receptor antagonist with important biological activity. It can inhibit 5-HT2B and has >1000-fold selectivity for 5-HT2B compared to other 5-HT receptors with a pKi of 9.5 and pIC50 of 10.4.
| Targets |
5-HT2B ( pIC50 = 10.4 ); 5-HT2B ( pIC50 = 9.5 )
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| Enzyme Assay |
Testing the compound's affinity at more than 100 additional ion channel or receptor binding sites allows researchers to determine how selective RS-127445 is for 5-HT2B receptors. 2 mM EDTA in phosphate buffered saline is used to harvest CHO-K1 cells expressing human 5-HT2A, 5-HT2B, or 5-HT2C receptors. The process involves four rounds of centrifugation (48,000×g for 15 min) and homogenization to prepare cell membranes. The purpose of every assay is to optimize specific binding and reach steady state conditions. The 5-HT2A receptor is detected by incubating membranes from 1×106 cells with 0.2 nM [3 H]-ketanserin for 60 minutes at 32 °C. We use 10 μM methysergide to measure nonspecific binding. 0.2 nM [3 H]-5-HT is incubated for 120 minutes at 48 °C on membranes from 1.5×106 cells in order to detect the 5-HT2B receptor. 10-fold increase in 5-HT is used to measure nonspecific binding. Membranes from 3x10^5 cells are incubated with 0.5 nM [3 H]-mesuler-gine at 32 °C for 60 minutes in order to detect the 5-HT2Creceptor. Ten micrograms of methysergide are used to measure nonspecific binding. Glass fiber filters (GF/B) that have been pretreated with 0.1% polyethylene imine are used to vacuum filter out samples to end assays. Liquid scintillation counting is used to calculate bound and total radioactivity. In all of these tests, specific binding of greater than 90% is attained.
|
||
| Cell Assay |
For 20 minutes at 37°C, 240 μl of HEK-293 cells expressing the human 5-HT2B receptor suspension are pre-incubated with RS-127445, vehicle, or other antagonists. HEK-293 cells are cultured in 162 cm2 flasks with [3H]-myoinositol (1.67 μCi/ml) in an inositol-free Hams F12 medium containing 10% dialyzed foetal bovine serum for an entire night at 37 °C. After being harvested, the cells are resuspended at a density of roughly 3×103 cells/ml in inositol-free Hams F12 media after being washed five times with phosphate buffered saline. The addition of 5-HT starts the reactions. After the reactions have lasted for sixty minutes, 50 μl of ice-cold 20% perchloric acid is added, the mixture is chilled in an ice-water bath for ten minutes, and 160 μl of 1 N KOH is neutralized. Two milliliters of room-temperature, 50 mM Tris-HCl (pH 7.4) are used to dilute each sample. After being cleaned with 5 ml of distilled water, the aqueous portion (2.2 ml) is transferred onto Dowex AG1X8 columns (1 ml, 1: 1, w/v). Following an 18 ml distilled water wash, 3 ml of 1 N HCl is used to elute the inositol phosphates from the columns. Using a Packard 1900CA analyzer, liquid scintillation spectroscopy is used to measure the eluted radioactivity.
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C17H16FN3
|
|
|---|---|---|
| Molecular Weight |
281.33
|
|
| Exact Mass |
281.13
|
|
| Elemental Analysis |
C, 72.58; H, 5.73; F, 6.75; N, 14.94
|
|
| CAS # |
199864-87-4
|
|
| Related CAS # |
RS-127445 hydrochloride; 199864-86-3
|
|
| Appearance |
Solid powder
|
|
| SMILES |
CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N
|
|
| InChi Key |
ZZZQXCUPAJFVBN-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C17H16FN3/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13/h3-10H,1-2H3,(H2,19,20,21)
|
|
| Chemical Name |
4-(4-fluoronaphthalen-1-yl)-6-propan-2-ylpyrimidin-2-amine
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
5%DMSO + Corn oil: 2.8mg/ml (9.95mM) (Please use freshly prepared in vivo formulations for optimal results.)
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5545 mL | 17.7727 mL | 35.5454 mL | |
| 5 mM | 0.7109 mL | 3.5545 mL | 7.1091 mL | |
| 10 mM | 0.3555 mL | 1.7773 mL | 3.5545 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.
|
|---|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
