ML204|cas:5465-86-1|西域试剂

ML204,99.08%

产品编号：Bellancom-12949| CAS NO：5465-86-1| 分子式：C₁₅H₁₈N₂| 分子量：226.32

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货号	价格	库存与货期
Bellancom-12949	￥500.00	杭州北京（现货）
Bellancom-12949	￥800.00	杭州北京（现货）
Bellancom-12949	￥1800.00	杭州北京（现货）
Bellancom-12949	￥2800.00	杭州北京（现货）

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ML204

产品介绍

ML204 是一个有效的、选择性的 TRPC4/TRPC5 通道的抑制剂，较 TRPC6 的选择性高出 19 倍，不影响其他的 TRP 通道和电压门控的钠、钾或 Ca²⁺ 通道。

生物活性

ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca²⁺ channels.

体外研究

ML204 inhibits TRPC4β-mediated intracellular Ca²⁺ rise with an IC₅₀ value of 0.96 μM (HEK293 cells) and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation.
ML204 blocks TRPC4β activity induced through either G_i/o stimulation by μ-opioid, 5HT_1A serotonin, and M₂ muscarinic receptors or G_q/11 stimulation by the endogenous M₃-like muscarinic receptors.
ML204 blocks LPS-induced TRPC5 channel activity.

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

体内研究

ML204 (1 mg/kg; s.c.; twice a day; for 5 days) causes mortality associated with exacerbated hypothermia and decreases peritoneal leukocyte numbers and cytokines in LPS-injected mice^[4].

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

Animal Model:	Nonfasted male C57BL/6 (2-3 months)^[4]
Dosage:	1 mg/kg
Administration:	Subcutaneous injection, twice a day, for 5 days (prior to LPS injection)
Result:	Induced mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response.

体内研究

ML204 (1 mg/kg; s.c.; twice a day; for 5 days) causes mortality associated with exacerbated hypothermia and decreases peritoneal leukocyte numbers and cytokines in LPS-injected mice^[4].

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

Animal Model:	Nonfasted male C57BL/6 (2-3 months)^[4]
Dosage:	1 mg/kg
Administration:	Subcutaneous injection, twice a day, for 5 days (prior to LPS injection)
Result:	Induced mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response.

性状

Oil

溶解性数据

In Vitro:

Ethanol : 50 mg/mL (220.93 mM; Need ultrasonic)

DMSO : ≥ 37 mg/mL (163.49 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	4.4185 mL	22.0926 mL	44.1852 mL
5 mM	0.8837 mL	4.4185 mL	8.8370 mL
10 mM	0.4419 mL	2.2093 mL	4.4185 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 (11.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (11.05 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 (11.05 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (11.05 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 (11.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (11.05 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。