ONO-8130 | CAS#459841-96-4 | EP1 receptor antagonist

ONO-8130
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 527859

CAS#: 459841-96-4

Description: ONO-8130 is an orally available EP1 receptor antagonist.

Chemical Structure

ONO-8130

CAS# 459841-96-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 527859
Name: ONO-8130
CAS#: 459841-96-4
Chemical Formula: C25H28N2O5S2
Exact Mass: 500.14
Molecular Weight: 500.628
Elemental Analysis: C, 59.98; H, 5.64; N, 5.60; O, 15.98; S, 12.81

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 180
5mg	USD 400
10mg	USD 660
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: ONO8130; ONO 8130; ONO-8130

IUPAC/Chemical Name: 4-[[[2,3-Dihydro-6-[(2-methylpropyl)[(4-methyl-2-thiazolyl)sulfonyl]amino]-1H-indene-5yl]oxy]methyl]benzoic acid

InChi Key: IOXMDBQCUCDLAF-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H28N2O5S2/c1-16(2)13-27(34(30,31)25-26-17(3)15-33-25)22-11-20-5-4-6-21(20)12-23(22)32-14-18-7-9-19(10-8-18)24(28)29/h7-12,15-16H,4-6,13-14H2,1-3H3,(H,28,29)

SMILES Code: O=C(O)C1=CC=C(COC2=CC3=C(CCC3)C=C2N(CC(C)C)S(=O)(C4=NC(C)=CS4)=O)C=C1

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:

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Biological target:	ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist.
In vitro activity:	Expression of mRNA for EP receptors and key enzymes in the PGE(2) pathway were assessed by real-time PCR using species-specific primers. Functional studies of GPT were performed in tissue organ baths. Expression of mRNA for the four EP receptors was found in airway smooth muscle. PGE(2) displayed a bell-shaped concentration-response curve, where the initial contraction was inhibited by the EP(1) receptor antagonist ONO-8130 and the subsequent relaxation by the EP(2) receptor antagonist PF-04418948. Reference: Br J Pharmacol. 2013 Feb;168(4):794-806. https://pubmed.ncbi.nlm.nih.gov/22934927/
In vivo activity:	Given the previous evidence for involvement of prostanoid EP1 receptors in facilitation of the bladder afferent nerve activity and micturition reflex, the present study investigated the effect of ONO-8130, a selective EP1 receptor antagonist, on cystitis-related bladder pain in mice. Oral preadministration of ONO-8130 at 0.3-30 mg/kg strongly prevented both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent manner, but had slight effect on the increased bladder weight and vascular permeability. Oral ONO-8130 at 30 mg/kg also reversed the established cystitis-related bladder pain. Intravesical administration of prostaglandin E2 caused prompt phosphorylation of ERK in the L6 spinal cord, an effect blocked by ONO-8130. Reference: Pain. 2011 Jun;152(6):1373-1381. https://pubmed.ncbi.nlm.nih.gov/21396778/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	1.0	2.00
	DMSO	26.5	52.99
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.00
	Ethanol	6.0	11.99

Preparing Stock Solutions

The following data is based on the product molecular weight 500.63 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. Säfholm J, Dahlén SE, Delin I, Maxey K, Stark K, Cardell LO, Adner M. PGE2 maintains the tone of the guinea pig trachea through a balance between activation of contractile EP1 receptors and relaxant EP2 receptors. Br J Pharmacol. 2013 Feb;168(4):794-806. doi: 10.1111/j.1476-5381.2012.02189.x. PMID: 22934927; PMCID: PMC3631371. 2. Miki T, Matsunami M, Nakamura S, Okada H, Matsuya H, Kawabata A. ONO-8130, a selective prostanoid EP1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. Pain. 2011 Jun;152(6):1373-1381. doi: 10.1016/j.pain.2011.02.019. Epub 2011 Mar 10. PMID: 21396778.
In vitro protocol:	1. Säfholm J, Dahlén SE, Delin I, Maxey K, Stark K, Cardell LO, Adner M. PGE2 maintains the tone of the guinea pig trachea through a balance between activation of contractile EP1 receptors and relaxant EP2 receptors. Br J Pharmacol. 2013 Feb;168(4):794-806. doi: 10.1111/j.1476-5381.2012.02189.x. PMID: 22934927; PMCID: PMC3631371.
In vivo protocol:	1. Miki T, Matsunami M, Nakamura S, Okada H, Matsuya H, Kawabata A. ONO-8130, a selective prostanoid EP1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. Pain. 2011 Jun;152(6):1373-1381. doi: 10.1016/j.pain.2011.02.019. Epub 2011 Mar 10. PMID: 21396778.

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1: Säfholm J, Dahlén SE, Adner M. Antagonising EP1 and EP2 receptors reveal that the TP receptor mediates a component of antigen-induced contraction of the guinea pig trachea. Eur J Pharmacol. 2013 Oct 15;718(1-3):277-82. doi: 10.1016/j.ejphar.2013.08.021. Epub 2013 Sep 5. PubMed PMID: 24012781.

2: Säfholm J, Dahlén SE, Delin I, Maxey K, Stark K, Cardell LO, Adner M. PGE2 maintains the tone of the guinea pig trachea through a balance between activation of contractile EP1 receptors and relaxant EP2 receptors. Br J Pharmacol. 2013 Feb;168(4):794-806. doi: 10.1111/j.1476-5381.2012.02189.x. PubMed PMID: 22934927; PubMed Central PMCID: PMC3631371.

3: Miki T, Matsunami M, Nakamura S, Okada H, Matsuya H, Kawabata A. ONO-8130, a selective prostanoid EP1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. Pain. 2011 Jun;152(6):1373-81. doi: 10.1016/j.pain.2011.02.019. Epub 2011 Mar 10. PubMed PMID: 21396778.

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