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MedKoo Cat#: 527859 | Name: ONO-8130
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Description:

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

ONO-8130 is an orally available EP1 receptor antagonist.

Chemical Structure

ONO-8130
ONO-8130
CAS#459841-96-4

Theoretical Analysis

MedKoo Cat#: 527859

Name: ONO-8130

CAS#: 459841-96-4

Chemical Formula: C25H28N2O5S2

Exact Mass: 500.1440

Molecular Weight: 500.63

Elemental Analysis: C, 59.98; H, 5.64; N, 5.60; O, 15.98; S, 12.81

Price and Availability

Size Price Availability Quantity
25mg USD 450.00 2 Weeks
100mg USD 1,250.00 2 Weeks
1g USD 4,650.00 2 Weeks
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Related CAS #
No Data
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
View handling instruction
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/
Solvent mg/mL 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
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

Recalculate based on batch purity %
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.
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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