LY2794193|cas:2173037-97-1|西域试剂

LY2794193,98.16%

产品编号：Bellancom-119243| CAS NO：2173037-97-1| 分子式：C₁₆H₁₈N₂O₆| 分子量：334.32

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-119243	￥5500.00	杭州北京（现货）
Bellancom-119243	￥8500.00	杭州北京（现货）
Bellancom-119243	￥28500.00	杭州北京（现货）
Bellancom-119243	￥39500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

LY2794193

产品介绍

LY2794193 是一种高效的选择性 mGlu3 受体激动剂 (hmGlu3 K_i=0.927 nM，EC₅₀=0.47 nM; hmGlu2 K_i=412 nM，EC₅₀=47.5 nM)。

生物活性

LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 K_i=0.927 nM，EC₅₀=0.47 nM; hmGlu2 K_i=412 nM，EC₅₀=47.5 nM).

体外研究

LY2794193 exhihits inhibition of spontaneous Ca²⁺ oscillations in cultured rat cortical neurons with an EC₅₀ of 43.6 nM.
In the rat cortical neuron Ca²⁺ oscillation assay, LY2794193 exhibits a biphasic inhibition of spontaneous Ca²⁺ transients (high affinity EC₅₀=0.44 nM; 48% of the total agonist response; low affinity EC₅₀=43.6 nM; 52% of the total agonist response) with combined maximal agonist efficacy (E_max) of 66%.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

LY2794193 (1-30 mg/kg, s.c.), given 30 min prior to PCP (5 mg/kg, s.c.) leads a dose-related reduction in ambulations.
LY2794193 (1 mg/kg; i.v.) exhibits moderate clearance (18.3 mL/min per kg) and volume of distribution (1.17 L/kg) with a calculated plasma half-life (T_1/2) of 3.1 h in Male Sprague-Dawley rats.
LY2794193 (3 mg/kg; s.c.) leads to the rapid appearance in the plasma (AUC=9.9 μM; C_max=6.78 μM; T_max=0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats
Dosage:	1, 3, 10, or 30 mg/kg
Administration:	Administrated s.c.; given 30 min prior to PCP (5 mg/kg, s.c.)
Result:	A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats
Dosage:	1, 3, 10, or 30 mg/kg
Administration:	Administrated s.c.; given 30 min prior to PCP (5 mg/kg, s.c.)
Result:	A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant.

性状

Solid

溶解性数据

In Vitro:

DMSO : 200 mg/mL (598.23 mM; Need ultrasonic)

H₂O : 2 mg/mL (5.98 mM; ultrasonic and adjust pH to 14 with NaOH)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9911 mL	14.9557 mL	29.9115 mL
5 mM	0.5982 mL	2.9911 mL	5.9823 mL
10 mM	0.2991 mL	1.4956 mL	2.9911 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (14.96 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (14.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (14.96 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (14.96 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。