4-DAMP - CAS:1952-15-4 - KKL Med Inc.

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4-DAMP (Synonyms:4-二苯乙酰氧基-N-甲基-哌啶甲碘化物;4-DAMP methiodide)

目录号 : KCM12307 CAS No. : 1952-15-4 纯度 : ≥98%

Data Sheet 产品使用指南

4-DAMP is a potent antagonist of the muscarinic M receptor (pK = 9.3). It is routinely used to study the regulation and functions of the M receptor. 4-DAMP also has a high affinity for the closely-related M receptor (pK = 8.9).

规格	价格	是否有货	数量
25mg		In-stock
50mg		In-stock
100mg		In-stock

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生物活性

4-DAMP is a potent and selective antagonist of M3 receptors and also has a high affinity for the closely-related M5 receptors. 4-DAMP combined with 5-Fluorouracil (5-Fu) could significantly reduce the cell viability and enhance apoptosis in MKN45 and BGC823 gastric cancer cells. 4-DAMP inhibits lipopolysaccharide (LPS)- and tobacco-induced pulmonary inflammation and reduces mucin 5AC (MUC5AC), oligomeric mucus/gel-forming secretion.

体外研究

The combination of 4-DAMP (10 μM, 5 days) and 5-Fu (5 μM, 5 days) can inhibit the growth of MKN45 and BGC823 cells and promote apoptosi.

Cell Viability Assay

Cell Line:	MKN45 and BGC823 cells
Concentration:	10 μM
Incubation Time:	5 days
Result:	Reduced the cell viability to (30±4.0)% and (35±6.0)% combined with 5-Fu in MKN45 and BGC823 cells, respectively.

体内研究

4-DAMP (1 mg/kg, once daily for 12 days) inhibits gastric tumor formation in nude mice bearing MKN45 and BGC823 tumor xenografts.
4-DAMP (0.6 or 0.12 mg/kg, intranasal instillation daily for 35 days) reduced AR symptom scores and nasal secretion weight, reversed goblet cell metaplasia, alleviated eosinophil infiltration, and inhibited levels of MUC5AC, histamine, cytokines, MMP9, and EGFR in allergic rhinitis (AR) guinea pigs.

Animal Model:	Mouse MKN45 and BGC823 tumor xenografts
Dosage:	1mg/kg
Administration:	i.p., daily for 12 days
Result:	Reduced the tumor sizes and the tumor weights in both MKN45 and BGC823 xenografts.

Animal Model:

AR guinea pigs

Dosage:

0.6 or 0.12 mg/kg

Administration:

intranasal instillation, daily for 35 days

Result:

Reduced the weights of nasal secretions, reversed goblet cell metaplasia of the animal nasal mucosal epithelium, inhibited the levels of MUC5AC mRNA, IL-4, IL-13, and TNF-α in AR guinea pigs.

分子式

C₂₁H₂₆NO₂^.I

分子量

451.34

CAS号

1952-15-4

中文名称

4-DAMP methiodide

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (221.56 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2156 mL	11.0781 mL	22.1562 mL
5 mM	0.4431 mL	2.2156 mL	4.4312 mL
10 mM	0.2216 mL	1.1078 mL	2.2156 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)。-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: ≥ 5 mg/mL (11.08 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.08 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 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% corn oil

Solubility: ≥ 5 mg/mL (11.08 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.08 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。