1176316-99-6

中文名称 1176316-99-6

英文名称 AgoMelatine (hydrochloride)

CAS 1176316-99-6

分子式 C15H18ClNO2

分子量 279.76

MOL 文件 1176316-99-6.mol

1176316-99-6 结构式

基本信息物理化学性质图谱信息 1176316-99-6价格(试剂级) 常见问题列表

基本信息

中文别名

盐酸阿戈美拉汀

英文别名

S-20098 HYDROCHLORIDE
AgoMelatine (hydrochloride)
Agomelatine hydrochloride (S-20098 hydrochloride)

所属类别

生物化工：激动剂抑制剂

物理化学性质

储存条件-20°C储存

溶解度DMSO: ≥ 100 mg/mL (357.45 mM)

形态粉末

颜色White to off-white

图谱信息

1176316-99-6(1176316-99-6)核磁图(¹HNMR)

1176316-99-6价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2024/04/30	HY-17038A	1176316-99-6 Agomelatine hydrochloride	1176316-99-6	5mg	460元
2024/04/30	HY-17038A	1176316-99-6 Agomelatine hydrochloride	1176316-99-6	10mM * 1mLin DMSO	506元
2024/04/30	HY-17038A	1176316-99-6 Agomelatine hydrochloride	1176316-99-6	10mg	714元

常见问题列表

生物活性

Agomelatine hydrochloride (S-20098 hydrochloride) 是一种 MT1 和 MT2 受体的特异性激动剂，对 CHO-hMT1，HEK-hMT1，CHO-hMT2，HEK-hMT2 的 Ki 分别为 0.1，0.06，0.12 和 0.27 nM。Agomelatine hydrochloride 还是一种选择性的 5-HT2C 受体拮抗剂，在天然 (猪) 和克隆的人 5-HT2C 受体中 pKi 分别为 6.4 和 6.2。

靶点

5-HT _2C Receptor

6.4 (pKi, native porcine)

5-HT _2C Receptor

6.2 (pKi, human)

hMT1

0.1 (Ki, CHO Cells)

hMT1

0.06 (Ki, HEK Cells)

hMT2

0.12 (Ki, CHO Cells)

hMT2

0.27 (Ki, HEK Cells)

体外研究

Agomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC ₅₀ s of 1.6±0.4, 0.10±0.04 nM for CHO hMT1 CHO-hMT2 (hΜΤ1 and hΜΤ2 receptors expressed in CHO or HEK cell membranes).
Agomelatine (S20098) also interacts with h5-HT2B receptors (6.6), whereas it shows low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors, and negligible (<5.0) affinity for other 5-HT receptors.

体内研究

Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls.

Animal Model:	Female Swiss mice (20-30 g) were administered PTZ (85 mg/kg, i.p.), PTX (7 mg/kg, i.p.), strychnine (75 mg/kg, i.p.), Pilocarpine (400 mg/kg, i.p.), respectively
Dosage:	25, 50, or 75 mg/kg
Administration:	Administered intraperitoneally (i.p.)
Result:	All dosages showed a significant decrease in thiobarbituric acid reactive substances (TBARS) levels and nitrite content in all brain areas when compared to controls in the Pilocarpine induced seizure model. All dosages decreased TBARS levels in all brain areas, and at low doses (25 or 50 mg/kg) decreased nitrite contents, but only at 25 or 50 mg/kg showed a significant increase in catalase activity in three brain areas when compared to controls in the Strychnine-induced seizure model. Did not have any antioxidant effects on parameters of oxidative stress produced by PTX- or PTZ-induced seizure models when compared to controls.