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AA92593
目录号 : KM3062 CAS No. : 457961-34-1 纯度 : 98%

AA92593 是选择性、竞争性的的 OPN4 (melanopsin) 拮抗剂。

规格 价格 是否有货 数量
5mg
In-stock
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

AA92593 is a selective and competitive OPN4 (melanopsin) antagonist.

体外研究

AA92593 is a competitive melanopsin antagonist, its presence in the retinal-binding pocket of melanopsin leads to the displacement of retinal, which could trigger a downstream signaling that would ultimately result in Per1 increased expression.
AA92593 is shown to be specific because it competes with retinaldehyde for the melanopsin retinal binding site which is very distinct from other opsins.
Inhibition of melanopsin activity with AA92593 increases a-MSH expression and induces melanin dispersion in the melanophores, which darkens the embryo.
AA92593 exhibits an IC50 of 665 nM in CHO cells.

Cell Viability Assay

Cell Line: Melan-a melanocytes and B16-F10 melanoma cells.
Concentration: 10 μM.
Incubation Time: 1 hour (heat 39.5 °C).
Result: Pharmacologically inhibited melanopsin.
体内研究

AA92593 is able to decrease IOP in rabbits living under normal light condition.
AA92593 produces an increment in melatonin levels resulting in a drop of IOP.

Animal Model: Wild type (WT) mice.
Dosage: 30 mg/kg.
Administration: IP 20 min prior to PLR measurement.
Result: Attenuated pupil constriction in response to light (10 ph.cm.s) by ~50%.
分子式
C13H19NO3S
分子量
269.36
CAS号
457961-34-1
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 : 250 mg/mL (928.13 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7125 mL 18.5625 mL 37.1250 mL
5 mM 0.7425 mL 3.7125 mL 7.4250 mL
10 mM 0.3713 mL 1.8563 mL 3.7125 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: ≥ 2.08 mg/mL (7.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.72 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.72 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (7.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.72 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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