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  3. ONO-8130

ONO-8130 是一种口服有效和选择性的前列腺素 EP1 受体 (EP1 receptor) 拮抗剂。ONO-8130 可阻断 L6 脊髓中 ERK 的磷酸化。ONO-8130 可减轻环磷酰胺致膀胱炎小鼠的膀胱疼痛。ONO-8130 可用于间质性膀胱炎的研究。

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ONO-8130 Chemical Structure

ONO-8130 Chemical Structure

CAS No. : 459841-96-4

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  • 生物活性

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  • 参考文献

生物活性

ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research[1].

体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

500.63

Formula

C25H28N2O5S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ONO-8130
目录号:
HY-110198
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