ER819762 | CAS#1155773-15-1 | E2 EP4 receptor Antagonist |MedKoo

ER819762
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531780

CAS#: 1155773-15-1

Description: ER819762 is a novel antagonist of the prostaglandin E2 EP4 receptor which inhibits Th1 differentiation and Th17 expansion.

Chemical Structure

ER819762

CAS# 1155773-15-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531780
Name: ER819762
CAS#: 1155773-15-1
Chemical Formula: C30H39N3O3
Exact Mass: 489.30
Molecular Weight: 489.660
Elemental Analysis: C, 73.59; H, 8.03; N, 8.58; O, 9.80

Price and Availability

Size	Price	Availability
5mg	USD 350	2 Weeks
10mg	USD 565	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: ER819762; ER 819762; ER-819762

IUPAC/Chemical Name: (5S)-1'-[(3,5-dimethylphenyl)methyl]-2-ethyl-6,8-dimethoxy-5-methylspiro[5,10-dihydroimidazo[1,5-b][2]benzazepine-3,4'-piperidine]-1-one

InChi Key: JHKJPRFJRFDWPD-QFIPXVFZSA-N

InChi Code: InChI=1S/C30H39N3O3/c1-7-32-29(34)26-9-8-24-17-25(35-5)18-27(36-6)28(24)22(4)33(26)30(32)10-12-31(13-11-30)19-23-15-20(2)14-21(3)16-23/h9,14-18,22H,7-8,10-13,19H2,1-6H3/t22-/m0/s1

SMILES Code: O=C1N(CC)C2(CCN(CC3=CC(C)=CC(C)=C3)CC2)N4C1=CCC5=CC(OC)=CC(OC)=C5[C@@H]4C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Potent EP4 receptor antagonist.
In vitro activity:	ER-819762 also suppressed human EP4 receptor-mediated cell signalling as measured in a cAMP-dependent reporter assay (IC50 value of 59 ± 6 nmol·L−1) (Fig. 1B). In a larger cell signalling panel of 107 GPCRs, ER-819762 (1 µmol·L−1) was highly selective for EP4 receptors, exhibiting no agonism or antagonism for any other receptor, including the related PGE2 EP1, EP2 and EP3 receptors (Table 1). Reference: Br J Pharmacol. 2010 May; 160(2): 292–310. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2874852/
In vivo activity:	This study first tested the effect of ER-819762 in the murine CIA model, an animal model widely used for assessing therapeutic agents for treatment of RA. When given orally prior to the onset of disease, ER-819762 dose-dependently suppressed the clinical signs of arthritis and delayed disease onset (Fig. 6A). ER-819762 also significantly suppressed disease progression when it was administered subsequent to the onset of disease (Fig. 6B). Furthermore, ER-819762 retarded bone erosion in the CIA model, as demonstrated by radiological evaluation (Fig. 6C). Reference: Br J Pharmacol. 2010 May; 160(2): 292–310. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2874852/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	1.0	2.00
	Ethanol	2.5	5.00

Preparing Stock Solutions

The following data is based on the product molecular weight 489.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Chen Q, Muramoto K, Masaaki N, Ding Y, Yang H, Mackey M, Li W, Inoue Y, Ackermann K, Shirota H, Matsumoto I, Spyvee M, Schiller S, Sumida T, Gusovsky F, Lamphier M. A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br J Pharmacol. 2010 May;160(2):292-310. doi: 10.1111/j.1476-5381.2010.00647.x. PMID: 20423341; PMCID: PMC2874852.
In vitro protocol:	1. Chen Q, Muramoto K, Masaaki N, Ding Y, Yang H, Mackey M, Li W, Inoue Y, Ackermann K, Shirota H, Matsumoto I, Spyvee M, Schiller S, Sumida T, Gusovsky F, Lamphier M. A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br J Pharmacol. 2010 May;160(2):292-310. doi: 10.1111/j.1476-5381.2010.00647.x. PMID: 20423341; PMCID: PMC2874852.
In vivo protocol:	1. Chen Q, Muramoto K, Masaaki N, Ding Y, Yang H, Mackey M, Li W, Inoue Y, Ackermann K, Shirota H, Matsumoto I, Spyvee M, Schiller S, Sumida T, Gusovsky F, Lamphier M. A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br J Pharmacol. 2010 May;160(2):292-310. doi: 10.1111/j.1476-5381.2010.00647.x. PMID: 20423341; PMCID: PMC2874852.

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1: Jones VC, Birrell MA, Maher SA, Griffiths M, Grace M, O'Donnell VB, Clark SR, Belvisi MG. Role of EP2 and EP4 receptors in airway microvascular leak induced by prostaglandin E2. Br J Pharmacol. 2016 Mar;173(6):992-1004. doi: 10.1111/bph.13400. PubMed PMID: 26639895; PubMed Central PMCID: PMC4831025.

2: Chen Q, Muramoto K, Masaaki N, Ding Y, Yang H, Mackey M, Li W, Inoue Y, Ackermann K, Shirota H, Matsumoto I, Spyvee M, Schiller S, Sumida T, Gusovsky F, Lamphier M. A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br J Pharmacol. 2010 May;160(2):292-310. doi: 10.1111/j.1476-5381.2010.00647.x. PubMed PMID: 20423341; PubMed Central PMCID: PMC2874852.

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