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RS-127445
別名：MT500
RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.
CAS No. 199864-87-4
文献中Selleckの製品使用例（4）
製品安全説明書
現在のバッチを見る：
S269801
DMSO]
56 mg/mL]
false]
Ethanol]
8 mg/mL]
false]
Water]
Insoluble]
false
純度：
98.72%
98.72
RS-127445関連製品
シグナル伝達経路
5-HT Receptor阻害剤の選択性比較
生物活性
| 製品説明 | RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors. | ||||
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| Targets |
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| In Vitro | ||||
| In vitro | RS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. This compound is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. It is thus among the highest affinity, most selective 5- HT2B receptor ligands. This chemical potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine. | |||
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| Kinase Assay | Radioligand binding | |||
| The selectivity of RS-127445 for 5-HT2B receptors is examined by testing this compound for affinity at over 100 additional ion channel or receptor binding sites. CHO-K1 cells expressing human 5-HT2A, 5-HT2B or 5-HT2C receptors are harvested using 2 mM EDTA in phosphate buffered saline. Cell membranes are prepared by four cycles of homogenization and centrifugation (48,000×g for 15 min). Each assay is established so as to achieve steady state conditions and to optimize specific binding. For the 5-HT2A receptor, membranes from 1×106 cells are incubated with 0.2 nM [3 H]-ketanserin at 32 °C for 60 min. Nonspecific binding is determined using 10 μM methysergide. For the 5-HT2B receptor, membranes from 1.5×106 cells are incubated with 0.2 nM [3 H]-5-HT at 48 °C for 120 min. Nonspecific binding is determined using 10 μM 5-HT. For the 5-HT2Creceptor, membranes from 3×10 5 cells are incubated with 0.5 nM [3 H]-mesuler -gine at 32 °C for 60 min. Nonspecific binding is determined using 10μM methysergide. Assays are terminated by vacuum filtration through glass fibre filters(GF/B) which has been pretreated with 0.1% polyethyleneimine. Total and bound radioactivity is determined by liquid scintillation counting. Greater than 90% specific binding is achieved in each of these assays. | ||||
| 細胞実験 | 細胞株 | HEK-293 cells expressing the human 5-HT2B receptor | ||
| 濃度 | 10 μM | |||
| 反応時間 | 20 min | |||
| 実験の流れ | RS-127445, vehicle or other antagonists are pre-incubated with 240 μl of HEK-293 cells expressing the human 5-HT2B receptor suspension at 37 °C for 20 min. HEK-293 cells are incubated with[3H]-myoinositol (1.67 μCi/ml) in 162 cm2 flasks overnight at 37 °C in an inositol free Ham's F12 medium containing 10% dialyzed foetal bovine serum. The cells are harvested, washed five times with phosphate bufffered saline and resuspended in inositol free Ham's F12 media at density of approximately 3×103 cells/ml. The reactions are initiated by addition of 5-HT. Sixty minutes later, the reactions are terminated by adding 50 μl of ice-cold 20% perchloric acid, chilled in an ice-water bath for 10 min and then neutralized with 160μl of 1 N KOH. Each sample is diluted with 2 ml of 50 mM Tris-HCl, pH 7.4 at room temperature. The aqueous portion (2.2 ml) is transferred onto Dowex AG1X8 columns (1 ml, 1 : 1, w/v) which has been washed with 5 ml of distilled water. The columns are then washed with 18 ml of distilled water and the inositol phosphates are eluted with 3 ml of 1 N HCl. The eluted radioactivity is determined by liquid scintillation spectroscopy using a Packard 1900CA analyzer. [1] |
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| In Vivo | ||
| In Vivo |
LD50: Mice 391.4mg/kg (i.v.); Rats 370.1mg/kg (i.v.); Rabbits 142.3mg/kg (i.v.) |
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| 動物実験 | 動物モデル | rats |
| 投与量 | 5 mg/kg | |
| 投与経路 | Oral for 2.5 h ,intraperitoneal and intravenousroutes for 0.08 h | |
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化学情報
| 分子量 | 281.33 | 化学式 | C17H16FN3 |
| CAS No. | 199864-87-4 | SDF | Download RS-127445 SDFをダウンロードする |
| Smiles | CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N | ||
| 保管 | |||
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In vitro |
DMSO : 56 mg/mL ( (199.05 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 8 mg/mL Water : Insoluble |
モル濃度計算器 |
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in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | |||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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