ONO-8130
- Product Name
- ONO-8130
- CAS No.
- 459841-96-4
- Chemical Name
- ONO-8130
- Synonyms
- ONO-8130;ONO-8130, 10 mM in DMSO;4-[[[2,3-Dihydro-6-[(2-methylpropyl)[(4-methyl-2-thiazolyl)sulfonyl]amino]-1H-indene-5yl]oxy]methyl]benzoic acid;Benzoic acid, 4-[[[2,3-dihydro-6-[(2-methylpropyl)[(4-methyl-2-thiazolyl)sulfonyl]amino]-1H-inden-5-yl]oxy]methyl]-;Orally active,ONO8130,Inhibitor,inhibit,Bladder pain,ONO 8130,Prostaglandin Receptor,Interstitial cystitis,PKR-like endoplasmic reticulum kinase,PERK,Hyperalgesia,Protein kinase R-like endoplasmic reticulum kinase,ONO-8130
- CBNumber
- CB43152708
- Molecular Formula
- C25H28N2O5S2
- Formula Weight
- 500.63
- MOL File
- 459841-96-4.mol
ONO-8130 Property
- Boiling point:
- 705.1±70.0 °C(Predicted)
- Density
- 1.344±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- ≤2mg/ml in ethanol;3mg/ml in DMSO;1mg/ml in dimethyl formamide
- form
- crystalline solid
- pka
- 4.17±0.10(Predicted)
N-Bromosuccinimide Price
- Product number
- 19118
- Product name
- ONO-8130
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $43
- Updated
- 2024/03/01
- Product number
- 19118
- Product name
- ONO-8130
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $178
- Updated
- 2024/03/01
- Product number
- 19118
- Product name
- ONO-8130
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $270
- Updated
- 2024/03/01
- Product number
- 19118
- Product name
- ONO-8130
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $621
- Updated
- 2024/03/01
- Product number
- 5406
- Product name
- ONO8130
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $1081
- Updated
- 2021/12/16
ONO-8130 Chemical Properties,Usage,Production
Uses
ONO 8130 is a selective prostanoid EP1 receptor antagonist, which relieves bladder pain in mice with cyclophosphamide-induced cystitis.
Biological Activity
ono-8130 is an orally bioavailable and selective antagonist of the prostaglandin e2 (pge2) receptor ep1 with ki value of 1.9 nm [1][2][3].prostaglandins contribute to the sensitization of peripheral and central nociceptive neurons during peripheral inflammation. prostaglandin e2 (pge2) is considered a dominant pronociceptive prostanoid. pge2 receptors are g protein-coupled receptors and classified into 4 general subtypes (ep1, ep2, ep3, and ep4) that are located unevenly in different tissues. ep1 receptors play a major role in processing of pain [1].in cystitis-related bladder pain 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 way. ono-8130 at 30 mg/kg also reversed the established cystitis-related bladder pain. ono-8130 also blocked prostaglandin e2 caused prompt phosphorylation of erk in the l6 spinal cord [1]. in the guinea pig trachea (gpt), ono-8130 inhibited the initial contraction mediated by pge2. ono-8130 also eliminated the spontaneous tone [2].
in vivo
ONO-8130 (0.3-30 mg/kg; Oral preadministration, once) strongly prevents both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent manner[1].
ONO-8130 (30 mg/kg; Orally, once) reverses the established cystitis-related bladder pain[1].
ONO-8130 (30 mg/kg; Orally, once) strongly inhibits phosphorylation of ERK in MDH, DCM, and SPN of the L6 spinal cord caused by intravesical administration of PGE2[1].
| Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old)[1] |
| Dosage: | 0.3, 3, 10, and 30 mg/kg |
| Administration: | Orally, once |
| Result: | 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. |
| Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old, established bladder pain caused by IP cyclophosphamide)[1] |
| Dosage: | 10, 30 mg/kg |
| Administration: | Orally, once (administered 2.75 hours after i.p. cyclophosphamide) |
| Result: | Markedly attenuated the bladder pain-like nociceptive behavior and referred hyperalgesia in the acute phase (3.5-4 h after cyclophosphamide). |
| Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old, established bladder pain caused by IP cyclophosphamide)[1] |
| Dosage: | 30 mg/kg |
| Administration: | Orally, once (administered 4.75 hours after i.p. cyclophosphamide) |
| Result: | Significantly suppressed the bladder pain-like nociceptive behavior and tended to reduce the referred hyperalgesia in the persistent phase, 5.5-6 hours after cyclophosphamide. |
| Animal Model: | Female ddY mice (18-22 g, 4-5 weeks old, intravesical administration of PGE2 at 5 nmol/mouse)[1] |
| Dosage: | 30 mg/kg |
| Administration: | Orally, once |
| Result: | Strongly inhibited phosphorylation of ERK in MDH, DCM, and SPN of the L6 spinal cord caused by intravesical administration of PGE2 at 5 nmol/mouse, exerted complete blockade in DCM, while its inhibitory effects in MDH and SPN were partial. |
storage
Store at +4°C
References
[1]. miki t, matsunami m, nakamura s, et al. ono-8130, a selective prostanoid ep1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. pain. 2011 jun;152(6):1373-81.
[2]. sfholm 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.
ONO-8130 Preparation Products And Raw materials
Raw materials
Preparation Products
ONO-8130 Suppliers
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- +86-0519-85788828 +86-13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 3934
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 15317229551
- Fax
- QQ:3607245178
- 15151849396@163.com
- Country
- China
- ProdList
- 989
- Advantage
- 58
- Tel
- 15869524721
- 3525679403@qq.com
- Country
- China
- ProdList
- 4989
- Advantage
- 58
- Tel
- 0371-0371-55135753 18003832934
- Fax
- QQ：2853979818
- 2853979818@qq.com
- Country
- China
- ProdList
- 9991
- Advantage
- 58
- Tel
- 13348960310
- 3003867561@qq.com
- Country
- China
- ProdList
- 10503
- Advantage
- 58
- Tel
- 15071299552
- Fax
- QQ:262933239
- 262933239@qq.com
- Country
- China
- ProdList
- 7047
- Advantage
- 58
- Tel
- 0371-86658258 ；0371-55969461
- Fax
- QQ：3311217266
- info@kehobio.com
- Country
- China
- ProdList
- 2575
- Advantage
- 58
- Tel
- 4008200310
- marketing@tsbiochem.com
- Country
- China
- ProdList
- 24961
- Advantage
- 58
- Tel
- 024-024-024-88590548 18341751992
- 757984502@qq.com
- Country
- China
- ProdList
- 942
- Advantage
- 58
- Tel
- 13720134139 086-15871494362 13720134139
- orders@jknbiochem.com
- Country
- China
- ProdList
- 6762
- Advantage
- 58
- Tel
- 0513-66337626 18051384581
- sales@chemhifuture.com
- Country
- China
- ProdList
- 5929
- Advantage
- 58
- Tel
- 13053322091
- admin@mopaikeji.com
- Country
- China
- ProdList
- 5830
- Advantage
- 58
- Tel
- 025-85560043 15850508050
- Fax
- 025-85563444
- cindy.huang@synzest.com
- Country
- China
- ProdList
- 12000
- Advantage
- 58
- Tel
- 13298105281
- 1522334715@qq.com
- Country
- China
- ProdList
- 7507
- Advantage
- 58
- Tel
- 0731-13823398 15111215862
- 313359644@qq.com
- Country
- China
- ProdList
- 4161
- Advantage
- 58
- Tel
- 17316404525 17316404525
- 209533805@qq.com
- Country
- China
- ProdList
- 9763
- Advantage
- 58
- Tel
- 18221172427
- sale@fine-biotech.com
- Country
- China
- ProdList
- 2746
- Advantage
- 58
- Tel
- 18003437475
- Fax
- 1-612-656-4400
- rdname@qq.com
- Country
- China
- ProdList
- 6960
- Advantage
- 58
- Tel
- 400-821-026
- Sales@sangon.com
- Country
- China
- ProdList
- 6710
- Advantage
- 58
- Tel
- 800-364-9897
- sales@caymanchem.com
- Country
- China
- ProdList
- 6838
- Advantage
- 58
- Tel
- 51288865780
- sales@biosynth.com
- Country
- China
- ProdList
- 6051
- Advantage
- 58
- Tel
- 400-025-6535
- sales@adooq.cn
- Country
- China
- ProdList
- 6215
- Advantage
- 58
- Tel
- +8613720134139
- orders@jknbiochem.com
- Country
- China
- ProdList
- 5221
- Advantage
- 58
- Tel
- +86-18341751992 +86-15382112998
- 757984502@qq.com
- Country
- China
- ProdList
- 892
- Advantage
- 58
- Tel
- +8618327326525
- masar@topule.com
- Country
- China
- ProdList
- 8467
- Advantage
- 58
- Tel
- 13102311730,18585291730
- Country
- CHINA
- ProdList
- 140
- Advantage
- 58
- Tel
- 19802084049
- Country
- CHINA
- ProdList
- 171
- Advantage
- 58
- Tel
- 020-83808789
- Country
- CHINA
- ProdList
- 179
- Advantage
- 58
- Tel
- --
- Fax
- --
- info@biorbyt.com
- Country
- CHINA
- ProdList
- 6482
- Advantage
- 58
- Tel
- --
- Fax
- --
- info@neobioscience.com
- Country
- CHINA
- ProdList
- 6207
- Advantage
- 58
- Tel
- --
- Fax
- --
- chenjw@absin.cn
- Country
- CHINA
- ProdList
- 6208
- Advantage
- 58
- Tel
- --
- Fax
- --
- Proteintech-CN@ptglab.com
- Country
- CHINA
- ProdList
- 6290
- Advantage
- 58
- Tel
- --
- Fax
- --
- info@zzsrm.com
- Country
- CHINA
- ProdList
- 6650
- Advantage
- 58
- Tel
- --
- Fax
- --
- 1985563437@qq.com
- Country
- CHINA
- ProdList
- 6525
- Advantage
- 58
- Tel
- --
- Fax
- --
- Country
- CHINA
- ProdList
- 6973
- Advantage
- 58
- Tel
- --
- Fax
- --
- 471161314@qq.com
- Country
- CHINA
- ProdList
- 6210
- Advantage
- 58
- Tel
- --
- Fax
- --
- 596799915@QQ.COM
- Country
- CHINA
- ProdList
- 2905
- Advantage
- 58