Ro 0437626
Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 134362-79-1
- 分子式: C27H35N5O4S
- 分子量:525.66
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
P2X Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
IC50: 3 μM (P2X1 receptor)
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
>100 μM
Compound: 1
|
Inhibitory concentration against human P2X purinoceptor 3 (hP2X3) expressed in CHO-K1 cells
Inhibitory concentration against human P2X purinoceptor 3 (hP2X3) expressed in CHO-K1 cells
|
[PMID: 15927468] |
| CHO-K1 | IC50 |
3 μM
Compound: 1
|
Inhibitory concentration against human P2X purinoceptor 1 (hP2X1) expressed in CHO-K1 cells
Inhibitory concentration against human P2X purinoceptor 1 (hP2X1) expressed in CHO-K1 cells
|
[PMID: 15927468] |
体外実験
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female rat (urethane-anaesthetized)[3]
-
Dosage:1 and 10 μmol/kg
-
Administration:I.v.
-
Result:Caused a reduction in postinfusion isovolumetric contractions.
化学情報
-
CAS 番号 134362-79-1
-
分子量 525.66
-
分子式 C27H35N5O4S
-
SMILES
O=C(C1=NC2=CC=CC=C2N1)N[C@H](CC3=CSC=N3)C(N[C@@H](CC4CCCCC4)[C@@H](O)[C@H](C5CC5)O)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
[1]. Jaime-Figueroa S, et al. Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist. Bioorg Med Chem Lett. 2005;15(13):3292-3295. [Content Brief]
[2]. Harper MT, et al. Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry. J Thromb Haemost. 2010;8(7):1604-1613. [Content Brief]
[3]. King BF, et al. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. Br J Pharmacol. 2004;142(3):519-530. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)