ENMD-1068 hydrochloride|cas:2703451-51-6|西域试剂

ENMD-1068 hydrochloride,98.18%

产品编号：Bellancom-124748A| CAS NO：2703451-51-6| 分子式：C₁₅H₃₀ClN₃O₂| 分子量：319.87

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货号	价格	库存与货期
Bellancom-124748A	￥950.00	杭州北京（现货）
Bellancom-124748A	￥1700.00	杭州北京（现货）
Bellancom-124748A	￥3500.00	杭州北京（现货）
Bellancom-124748A	￥6000.00	杭州北京（现货）

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ENMD-1068 hydrochloride

产品介绍

ENMD-1068 hydrochloride 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride可通过抑制 TGF-β1/Smad 信号转导而减少肝星状细胞的活化和胶原蛋白的表达。ENMD-1068 hydrochloride 还能抑制子宫内膜细胞的增殖，并诱导病灶中上皮细胞的凋亡。ENMD-1068 hydrochloride 可用于子宫内膜异位症、肝纤维化的研究。

生物活性

ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.

体外研究

ENMD-1068 (10 mM; 24 h) blocks TGF-β1/Smad signaling in primary mouse HSCs (TGF-β1/Smad signal pathway plays a crucial role in HSCs activation and collagen production).
ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs.

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

Western Blot Analysis

Cell Line:	Hepatic stellate cells (HSCs) (TGF-β1-stimulated)
Concentration:	10 mM
Incubation Time:	24 h
Result:	Inhibited TGF-β1-induced expression of α-SMA, Col α1(І),Col α1(III), and Smad2/3 C-terminal phosphorylation.

体内研究
(In Vivo)

ENMD-1068 (25, 50 mg/kg; i.p.; twice per week for 4 weeks) inhibits liver fibrosis of mice.
ENMD-1068 (25, 50 mg/kg; i.p.; single daily for 5 days) inhibits endometriosis growth and suppresses the levels of IL-6 and MCP-1 in a dose-dependent manner.
ENMD-1068 (25, 50 mg/kg; i.p.; single daily for 5 days) causes a decrease in epithelial cell proliferation and an increase in the apoptotic index in mice.

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

Animal Model:	ICR mice (8-week-old; CCl₄-induced liver fibrosis model).
Dosage:	25, 50 mg/kg
Administration:	Intraperitoneal injection; twice per week for 4 weeks
Result:	Markedly attenuated collagen deposition.

Animal Model:	Mice with surgically induced endometriosis.
Dosage:	25, 50 mg/kg
Administration:	Intraperitoneal injection; single daily for 5 days
Result:	Reduced the volume of observed lesions in a dose-dependent manner. Inhibited the expression of IL-6 and MCP-1. Decreased the proliferation rate of endometriotic cells and increased the percentage of apoptotic epithelial cells in the lesions.

体内研究

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

Animal Model:	ICR mice (8-week-old; CCl₄-induced liver fibrosis model).
Dosage:	25, 50 mg/kg
Administration:	Intraperitoneal injection; twice per week for 4 weeks
Result:	Markedly attenuated collagen deposition.

Animal Model:	Mice with surgically induced endometriosis.
Dosage:	25, 50 mg/kg
Administration:	Intraperitoneal injection; single daily for 5 days
Result:	Reduced the volume of observed lesions in a dose-dependent manner. Inhibited the expression of IL-6 and MCP-1. Decreased the proliferation rate of endometriotic cells and increased the percentage of apoptotic epithelial cells in the lesions.

体内研究

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

Animal Model:	ICR mice (8-week-old; CCl₄-induced liver fibrosis model).
Dosage:	25, 50 mg/kg
Administration:	Intraperitoneal injection; twice per week for 4 weeks
Result:	Markedly attenuated collagen deposition.

Animal Model:	Mice with surgically induced endometriosis.
Dosage:	25, 50 mg/kg
Administration:	Intraperitoneal injection; single daily for 5 days
Result:	Reduced the volume of observed lesions in a dose-dependent manner. Inhibited the expression of IL-6 and MCP-1. Decreased the proliferation rate of endometriotic cells and increased the percentage of apoptotic epithelial cells in the lesions.

性状

Solid

溶解性数据

In Vitro:

DMSO : 200 mg/mL (625.25 mM; Need ultrasonic)

H₂O : 100 mg/mL (312.63 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1263 mL	15.6314 mL	31.2627 mL
5 mM	0.6253 mL	3.1263 mL	6.2525 mL
10 mM	0.3126 mL	1.5631 mL	3.1263 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 (stored under nitrogen)。-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： PBS
Solubility: 100 mg/mL (312.63 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 5 mg/mL (15.63 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (15.63 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 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。
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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (15.63 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 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (15.63 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。