RO27-3225 TFA

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RO27-3225 TFA; 纯度: 99.57%

RO27-3225 TFA 是一种有效的选择性黑皮质素 4 受体 (MC4R) 激动剂，对于 MC4R 和 MC1R 的 EC50 分别为 1 nM 和 8 nM。RO27-3225 TFA 对 MC4R 的选择性是 MC3R 的 30 倍左右。RO27-3225 TFA 具有神经保护和抗炎作用。

RO27-3225 TFAamp;;

RO27-3225 TFA Chemical Structure

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥4750 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
50 mg ￥13500 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

RO27-3225 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Neuronal Signaling Compound Library
  • Neuroprotective Compound Library
  • Anti-Obesity Compound Library
  • Peptide Library

生物活性

RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects[1][2][3].

IC50 Target

EC50: 1 nM (Melanocortin 4 receptor (MC4R)), 8 nM (MC1R), 675 nM (MC3R) and 5779 nM (MC5R)[1]
体内研究
(In Vivo)

RO27-3225 (0.012-0.048 mg/kg; intravenous injection; Wistar rats) treatment reverses haemorrhagic shock, reduces multiple organ damage and improves survival. RO27-3225 could have a protective role against multiple organ failure following circulatory shock[2].

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

Animal Model: Wistar rats of both sexes (270-300 g) with haemorrhagic shock[2]
Dosage: 0.012 mg/kg, 0.024 mg/kg, 0.048 mg/kg
Administration: Intravenous injection
Result: Reversed haemorrhagic shock, reduced multiple organ damage and improved survival.

分子量

898.93

Formula

C41H53F3N12O8
Sequence

Oxobutyl-His-Phe-Arg-Trp-{Sar}-NH2
Sequence Shortening

Oxobutyl-HFRW-{Sar}-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:;

H2O : 100 mg/mL (111.24 mM; Need ultrasonic)

DMSO : 100 mg/mL (111.24 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1124 mL 5.5622 mL 11.1243 mL
5 mM 0.2225 mL 1.1124 mL 2.2249 mL
10 mM 0.1112 mL 0.5562 mL 1.1124 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 (sealed storage, away from moisture and light)。-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 (2.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.78 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。

    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-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.78 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 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
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (2.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.78 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 MCE 网站选购。
参考文献

  • [1]. Benoit SC, et al. A novel selective melanocortin-4 receptor agonist reduces food intake in rats and mice without producing aversive consequences. J Neurosci. 2000 May 1;20(9):3442-8.

    [2]. Giuliani D, et al. Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br J Pharmacol. 2007 Mar;150(5):595-603.

    [3]. Zhang Y, et al. Effects of RO27-3225 on neurogenesis, PDGFRβ+ cells and neuroinflammation after cerebral infarction. Int Immunopharmacol. 2020 Feb 11;81:106281.