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Agomelatine(L(+)-Tartaric acid)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Agomelatine(L(+)-Tartaric acid)图片
CAS NO:824393-18-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
阿戈美拉汀 L(+)-酒石酸
S-20098 L(+)-Tartaric acid
产品介绍
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) 是一种MT1MT2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 L(+)-Tartaric acid 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。
生物活性

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist ofMT1andMT2receptors withKis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine L(+)-Tartaric acid is a selective5-HT2C receptorantagonist withpKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

IC50& Target

MT2

 

MT1

 

5-HT2CReceptor

6.4 (pKi, native porcine)

5-HT2CReceptor

6.2 (pKi, human)

hMT1

0.1 nM (Ki, CHO Cells)

hMT1

0.06 nM (Ki, HEK Cells)

hMT2

0.12 nM (Ki, CHO Cells)

hMT2

0.27 nM (Ki, HEK Cells)

体外研究
(In Vitro)

Agomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC50s 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)[1].
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[2].

体内研究
(In Vivo)

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[3].

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[3]
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.
Clinical Trial
分子量

393.39

性状

Solid

Formula

C19H23NO8

CAS 号

824393-18-2

中文名称

阿戈美拉汀 L(+)-酒石酸;维度新 L(+)-酒石酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(254.20 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5420 mL12.7100 mL25.4201 mL
5 mM0.5084 mL2.5420 mL5.0840 mL
10 mM0.2542 mL1.2710 mL2.5420 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: 2.5 mg/mL (6.36 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.36 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.36 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.36 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。