ENMD-1068 hydrochloride

Name: ENMD-1068 hydrochloride
Brand: MedChemExpress
SKU: HY-124748A
Rating: 5.0 (2 reviews)

製品番号: HY-124748A 純度: 98.33%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

ENMD-1068 hydrochloride 構造式

CAS 番号 : 2703451-51-6

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 104	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 104	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$95	在庫あり	Estimated Time of Arrival: December 31
10 mg	$170	在庫あり	Estimated Time of Arrival: December 31
25 mg	$350	在庫あり	Estimated Time of Arrival: December 31
50 mg	$600	在庫あり	Estimated Time of Arrival: December 31
100 mg		お問い合わせ
200 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Other Forms of ENMD-1068 hydrochloride:

ENMD-1068 hydrobromide お問い合わせ
ENMD-1068 お問い合わせ

顧客検証

Protease Activated Receptor (PAR) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PAR1 PAR2 PAR4

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

PAR2

体外実験

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)^[1].
ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs^[1].

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

Western Blot Analysis^[1]

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.

体内実験

ENMD-1068 (25, 50 mg/kg; i.p.; twice per week for 4 weeks) inhibits liver fibrosis of mice^[1].
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^[2].
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^[2].

MedChemExpress (MCE) 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)^[1].
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^[2].
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.

分子量

319.87

分子式

C₁₅H₃₀ClN₃O₂

CAS 番号

2703451-51-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C(CC(C)C)=O)CC1)CCCCCN.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶剤 & 溶解度

体外:

DMSO : 200 mg/mL (625.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (15.63 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (312.63 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 98.33%

Select Batch:

データシート (275 KB) SDS (392 KB)

COA (243 KB) HNMR (257 KB) RP-HPLC (243 KB) LCMS (87 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Sun Q, et al. ENMD-1068 inhibits liver fibrosis through attenuation of TGF-β1/Smad2/3 signaling in mice. Sci Rep. 2017 Jul 14;7(1):5498. doi: 10.1038/s41598-017-05190-7. Erratum in: Sci Rep. 2019 Dec 10;9(1):19125. [Content Brief]

[2]. Wang Y, et al. ENMD-1068, a protease-activated receptor 2 antagonist, inhibits the development of endometriosis in a mouse model. Am J Obstet Gynecol. 2014 Jun;210(6):531.e1-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.1263 mL	15.6314 mL	31.2627 mL	78.1568 mL
	5 mM	0.6253 mL	3.1263 mL	6.2525 mL	15.6314 mL
	10 mM	0.3126 mL	1.5631 mL	3.1263 mL	7.8157 mL
	15 mM	0.2084 mL	1.0421 mL	2.0842 mL	5.2105 mL
	20 mM	0.1563 mL	0.7816 mL	1.5631 mL	3.9078 mL
	25 mM	0.1251 mL	0.6253 mL	1.2505 mL	3.1263 mL
	30 mM	0.1042 mL	0.5210 mL	1.0421 mL	2.6052 mL
	40 mM	0.0782 mL	0.3908 mL	0.7816 mL	1.9539 mL
	50 mM	0.0625 mL	0.3126 mL	0.6253 mL	1.5631 mL
	60 mM	0.0521 mL	0.2605 mL	0.5210 mL	1.3026 mL
	80 mM	0.0391 mL	0.1954 mL	0.3908 mL	0.9770 mL
	100 mM	0.0313 mL	0.1563 mL	0.3126 mL	0.7816 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.