LY2794193 是一种高效的选择性mGlu3受体激动剂 (hmGlu3Ki=0.927 nM，EC50=0.47 nM;hmGlu2Ki=412 nM，EC50=47.5 nM)。
| 生物活性 | LY2794193 is a highly potent and selectivemGlu3 receptoragonist (hmGlu3Ki=0.927 nM，EC50=0.47 nM;hmGlu2Ki=412 nM，EC50=47.5 nM)[1]. |
| IC50& Target[1] | mGluR3 0.47 nM (EC50) | mGluR3 0.927 nM (Ki) | mGluR2 47.5 (EC50) | mGluR2 412 (Ki) |
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体外研究
(In Vitro) | LY2794193 exhihits inhibition of spontaneous Ca2+oscillations in cultured rat cortical neurons with an EC50of 43.6 nM[1].
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 (Emax) of 66%[1].
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体内研究
(In Vivo) | 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[1].
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 (T1/2) of 3.1 h in Male Sprague-Dawley rats[1].
LY2794193 (3 mg/kg; s.c.) leads to the rapid appearance in the plasma (AUC=9.9 μM; Cmax=6.78 μM; Tmax=0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats[1].
| 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. |
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| 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 |
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| 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 | 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℃, 6 months; -20℃, 1 month。-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 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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。
*以上所有助溶剂都可在本网站选购。 |
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