[CAS NO. 475085-57-5] MRE-269 (ACT-333679)

Name: MRE-269 (ACT-333679)
Brand: Arctom Scientific
SKU: SLK-S5819

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PRODUCTS SPECIFICATIONS [475085-57-5]

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Catalog

SLK-S5819

Brand

Selleck

CAS

475085-57-5

DESCRIPTION [475085-57-5]

Overview

MDL	MFCD11976884
Molecular Weight	419.52
Molecular Formula	C25H29N3O3
SMILES	N(CCCCOCC(O)=O)(C(C)C)C=1N=C(C(=NC1)C2=CC=CC=C2)C3=CC=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3837 mL	11.9184 mL	23.8368 mL
5 mM	0.4767 mL	2.3837 mL	4.7674 mL
10 mM	0.2384 mL	1.1918 mL	2.3837 mL
50 mM	0.0477 mL	0.2384 mL	0.4767 mL

Description

MRE-269 (ACT-333679) is a agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.

Targets

human IP receptor ^[1]

20 nM(Ki)

In vitro

MRE-269 bound to the human IP receptor with high affinity (binding affinity (Ki) of 20 nM) and with more than 130-fold selectivity over other prostanoid receptors (prostaglandin E receptors, EP1−4; prostaglandin D receptor, DP1; prostaglandin F2 receptor, FP; thromboxane A2 receptor, TP). In pulmonary arterial smooth muscle cells (PASMCs), MRE-269 potently induces accumulation of intracellular cAMP, leading to long-lasting (>10 h) membrane hyperpolarization (EC50 = 32 nM) which contributes to cell relaxation. It also causes long-lasting and pronounced relaxation of PASMCs.

In vivo

After Oral Administration (1 mg/kg) to monkeys, the T (time to reach maximum observed plasma concentration), C (maximum observed plasma concentration), AUC (area under the curve from 0 to 24 h after dosing) and T (apparent terminal half-life) are 2.3 h, 105 ng/mL, 652 ng·h/mL and 5.6 h, respectively for MRE-269.

References

[1] Asaki T, et al. J Med Chem. 2015, 58(18):7128-37.

Synonyms

Acetic acid, 2-[4-[(5,6-diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]-

Acetic acid, [4-[(5,6-diphenylpyrazinyl)(1-methylethyl)amino]butoxy]-

2-[4-[(5,6-Diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]acetic acid

MRE 269

ACT 333679

[4-[(5,6-Diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]acetic acid

2-[4-[(5,6-Diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy]acetic acid

2-(4-((5,6-Diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid