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MRE-269 (ACT-333679) - 10mM in DMSO, high purity , CAS No.475085-57-5

  • Moligand™
  • 10mM in DMSO
Item Number
M424131
Grouped product items
SKUSizeAvailabilityPrice Qty
M424131-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$241.90

Prostaglandin Receptor Agonists

Basic Description

SynonymsMRE-269|475085-57-5|ACT-333679|MRE269|MRE 269|ACT 333679|(4-((5,6-Diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid|2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid|E9PC7N0DID|CHEMBL239226|ACT333679|2-[4-[(5,6-diphenylpyrazin-2-y
Specifications & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsMRE-269 (ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

Information

MRE-269 (ACT-333679) MRE-269 (ACT-333679) is a prostaglandin I2 (IP) receptor 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 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 Tmax (time to reach maximum observed plasma concentration), Cmax (maximum observed plasma concentration), AUC0−24h (area under the curve from 0 to 24 h after dosing) and T1/2 (apparent terminal half-life) are 2.3 h, 105 ng/mL, 652 ng·h/mL and 5.6 h, respectively for MRE-269.

Names and Identifiers

IUPAC Name 2-[4-[(5,6-diphenylpyrazin-2-yl)-propan-2-ylamino]butoxy]acetic acid
INCHI InChI=1S/C25H29N3O3/c1-19(2)28(15-9-10-16-31-18-23(29)30)22-17-26-24(20-11-5-3-6-12-20)25(27-22)21-13-7-4-8-14-21/h3-8,11-14,17,19H,9-10,15-16,18H2,1-2H3,(H,29,30)
InChi Key OJQMKCBWYCWFPU-UHFFFAOYSA-N
Canonical SMILES CC(C)N(CCCCOCC(=O)O)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
Isomeric SMILES CC(C)N(CCCCOCC(=O)O)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
PubChem CID 9931891
Molecular Weight 419.52

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