[CAS NO. 2703451-51-6] ENMD-1068hydrochloride

Name: ENMD-1068hydrochloride
Brand: Arctom Scientific
SKU: HY-124748A

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [2703451-51-6]

Store

Catalog

HY-124748A

Brand

MCE

CAS

2703451-51-6

DESCRIPTION [2703451-51-6]

Overview

MDL	-
Molecular Weight	319.87
Molecular Formula	C15H30ClN3O2
SMILES	O=C(N1CCN(C(CC(C)C)=O)CC1)CCCCCN.Cl

For research use only. We do not sell to patients.

Summary

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 ^[1] ^[2] .

IC50 & Target

PAR2

In Vitro

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] .

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.

In Vivo

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] .

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

Animal Model:	ICR mice (8-week-old; CCl ₄ -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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

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

H ₂ O : 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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 100 mg/mL (312.63 mM); Clear solution; Need ultrasonic
2.

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
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution

* All of the co-solvents are available by MCE.