VU0364770 - CAS:61350-00-3

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VU0364770

目录号 : KM9597 CAS No. : 61350-00-3 纯度 : 98%

Data Sheet 产品使用指南

VU0364770 是一种有效的选择性 mGlu4 正变构调节剂 (PAM)。VU0346770 对大鼠 mGlu4 和人 mGlu4 受体的 EC₅₀ 分别为 290 nM 和 1.1 μM。VU0364770 对 mGlu5 具有拮抗活性，EC₅₀ 为 17.9 μM，VU0364770 对 mGlu6 具有正变构调节活性，EC₅₀ 为 6.8 μM。VU0364770 还对 MAO 具有活性，作用于人 MAO-A 和 MAO-B 的 K_i 值分别为8.5 和 0.72 μM。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC₅₀s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.

体外研究

VU0364770 is a selective positive allosteric modulator of mGlu₄ in recombinant systems. VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu₄ receptors to the endogenous agonist glutamate. VU0364770 produces a concentration-dependent potentiation of the response to an EC₂₀ concentration of glutamate with EC₅₀ of 1.1±0.2 μM and increases the maximal response to glutamate from 100 to 227±17%. Because of concerns that this chemical scaffold might possess activity at MAO, full IC₅₀ determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms; these studies result in K_is of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively. When tested at a 10 μM concentration at each mGlu receptor, VU0364770 exhibits weak PAM activity (4.3-fold left shift of the glutamate CRC) at mGlu6 and antagonist activity (3.3-fold right shift of the glutamate CRC) at mGlu5 (compare to the 16.5-fold left shift of the glutamate concentration-response for mGlu₄ at 10 μM). When further evaluated in a full concentration-response curve format, VU0364770 exhibits antagonist activity at mGlu₅ with a potency of 17.9±5.5 μM and PAM activity at mGlu₆ with a potency of 6.8±1.7 μM (compare with the potency of VU0364770 on the rat mGlu₄ receptor of 290±80 nM).

体内研究

VU0364770 exhibits suitable pharmacokinetic properties for systemic dosing in animal models. After intravenous administration, VU0364770 is rapidly clears from the systemic circulation (165 ml/min/kg) and exhibits a volume of distribution of 2.92 L/kg. VU0364770 is a highly protein-bound ligand displaying free fractions of 2.7 and 1.8% in human and rat plasma, respectively. VU0364770 also shows an improved pharmacokinetic profile relative to previously reported mGlu₄ PAMs with enhanced central penetration and a total brain-to-plasma ratio of more than 1 after systemic administration of a 10 mg/kg dose. VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy. VU0364770 dose-dependently reverses haloperidol (0.75 mg/kg)-induced catalepsy in rats, significant at doses of 10 to 56.6 mg/kg, after subcutaneous dosing (F_6,69=8.04; p<0.001).

分子式

C₁₂H₉ClN₂O

分子量

232.67

CAS号

61350-00-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (429.79 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.2979 mL	21.4897 mL	42.9793 mL
5 mM	0.8596 mL	4.2979 mL	8.5959 mL
10 mM	0.4298 mL	2.1490 mL	4.2979 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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 (10.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.74 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 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.74 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。