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| CAS号: | 273404-37-8 |
| 英文名称: | Belnacasan (VX-765) |
| 英文同义词: | VX-765(Belnacasan);Belnacasan (VX765);N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide;N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide VX 765;(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide |
| 中文名称: | Belnacasan (VX-765) |
| 中文同义词: | N-(4-氨基-3-氯苯甲酰基)-3-甲基-L-缬氨酰-N-[(2R,3S)-2-乙氧基四氢-5-氧代-3-呋喃基]-L-脯氨酰胺 |
| CBNumber: | CB72513725 |
| 分子式: | C24H33ClN4O6 |
| 分子量: | 508.99502 |
| MOL File: | 273404-37-8.mol |
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Belnacasan (VX-765) 性质、用途与生产工艺 |
生物活性
VX-765是一种有效的选择性的caspase-1抑制剂， Ki为0.8 nM。Phase 2。
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体外研究
VX-765 is an orally absorbed prodrug of VRT-043198, which exhibits potent inhibition against ICE/caspase-1 and caspase-4 with Ki of 0.8 nM and less than 0.6 nM, respectively. And VRT-043198 also inhibits IL-1β release from both PBMCs and whole blood with IC50 of 0.67 μM and 1.9 μM, respectively.
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体内研究
In collagen-induced arthritis mouse model, VX-765 (200 mg/kg) inhibits LPS-induced IL-1β production by about 60%, and results in a dose-dependent, statistically significant reduction in the inflammation scores and effective protection from joint changes. In vivo, VX-765 blocks kindling epileptogenesis in rats by preventing IL-1β increase in forebrain astrocytes without significant effect on afterdischarge duration. In the mouse model of acute seizures, VX-765 (50 mg/kg-200 mg/kg) produces the anticonvulsant effect by delaying the time to onset of the first seizure and decreasing the number of seizures as well as their total duration by average 50% and 64%. In adult rats with genetic absence epilepsy (GAERS), VX-765, after the 3rd drug injection, significantly reduces the cumulative duration and number of spike-and-wave discharges (SWDs) by 55% on average by selectively blocking IL-1β biosynthesis.
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特征
VX-765 is a potent and selective inhibitor of interleukin-converting enzyme/caspase-1.
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| Belnacasan (VX-765) 上下游产品信息 |
上游原料
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下游产品
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| Belnacasan (VX-765) 生产厂家 全球有 33家供应商
Belnacasan (VX-765)国内生产厂家
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| 供应商 | 联系电话 | 传真 | 电子邮件 | 国家 | 产品数 | 优势度 |
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上海永璨生物科技有限公司
| 0086-27-5925 3327; QQ:40199614 | 0086-27-5925 3326 | sales@sun-shinechem.com | 中国 |
302
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64
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上海波以尔化工有限公司
| Mr Qiu 86-21-50182298(Domestic Market)Miss Xu 86-21-50180596(Abroad Market) | 86-21-57758967 | sales@boylechem.com | 中国 |
5604
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55
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百灵威科技有限公司
| -- | -- | jkinfo@jkchemical.com;market3@jkchemical.com | 中国 |
96847
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76
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Shangchem Co., Ltd.
| +86-21-68182121，+86 15000169545 | +86-21-68182121 | steven@shangchem.com | 中国 |
882
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52
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南京康满林化工实业有限公司
| 025-83697070; 010-68547217 | +86-25-83453306 | sales@chemlin.com.cn | 中国 |
20120
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64
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凯试（上海）科技有限公司
| 021-50135380 | | shchemsky@sina.com | 中国 |
32553
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50
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ShangHai Biochempartner Co.,Ltd
| +86 13818785766，400-021-9906 | | gaoqing@biochempartner.com | 中国 |
1167
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62
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BOC Sciences
| 1-631-504-6093 | 1-631-614-7828 | sales@bocsci.com | 美国 |
9972
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65
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Wuhan NCE Biomedical Co.,Ltd.
| 4000-027-021 |24 hour enquiry :+86-13986109188 |English:+86-15623472865 |Japanese:+81-08033611988 | +86-27-87599188 | sales@ncebiomed.com | 中国 |
1503
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55
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上海皓元化学科技有限公司
| 86-21-58998590 | 86-21-53700326, 86-21-58998590 | sales@chemexpress.cn | 中国 |
10011
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61
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MedChemexpress LLC
| 609-228-6898 | 609-228-5909 | sales@medchemexpress.cn | 美国 |
4935
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58
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Shanghai Witofly Chemical Co.,Ltd
| | | sales@witofly.com | 中国 |
2877
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52
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AdooQ BioScience, LLC
| +1 (866) 930-6790 | +1 (866) 333-9607 | info@adooq.com | 美国 |
2786
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58
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上海智存生物科技有限公司
| +86-021-31135716 13761914825 | +86-021-61624218 | wulesian@wulechem.com sales@wulechem.com QQ 409132824 | 中国 |
271
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58
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CEG Chemical Science&Technology Co., Ltd.
| Mobile:13665161512 | +86-510-68873513 | sales@cegchem.com | 中国 |
2050
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58
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无锡嘉乐医药有限公司
| +86 (510) 86396359 13382276200 | +86 (510) 86396359 | sales@jalor-chem.com | 中国 |
497
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56
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上海寰川实业有限公司
| 021-61478794 | 021-61478794 | sales@hcshhai.com | 中国 |
9824
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50
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南京百鑫德诺生物科技有限公司
| 400-025-6535 | 025-68650336 | info@adooq.cn | 中国 |
2299
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60
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上海孚一生物科技有限公司
| +86 (21) 61124340 | +86 (21) 6129-4103 | sales02@forever-reagent.com | 中国 |
9802
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58
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湖北巨胜科技有限公司
| North:027-59599241,18871490274,QQ:1400878000 South:027-59531287,15727001360,QQ:1400878866 | ℡ 027-83861211 | 469501031@qq.com | 中国 |
10512
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58
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上海惯承化工科技有限公司
| Please Email：sales@letopharm.com | +86-21-5106 2861 | sales@letopharm.com | 中国 |
2641
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58
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上海楼岚生物科技有限公司
| +86-21-61128122 | +86-21-61128122 | sales@lollanechem.com | 中国 |
991
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55
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上海泽涵生物医药科技有限公司
| 0086-021-61350663 13052117465 | 0086-021-61350662 | sales@zehanbiopharma.com | 中国 |
498
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广州致雅医药科技有限公司
| 18122150900 | QQ：2377102418 | sales@greenchemdrug.com | 中国 |
809
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55
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斯派螺（武汉）药物研发有限公司
| | - | eric_feng1954@126.com | 中国 |
9716
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55
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上海升德医药科技有限公司
| 021-50266790 13585868794 QQ2635253576, 2086672224 | 021-50266790 | sale@shsendpharm.com | 中国 |
1898
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C24H33ClN4O6
N-(4-氨基-3-氯苯甲酰基)-3-甲基-L-缬氨酰-N-[(2R,3S)-2-乙氧基四氢-5-氧代-3-呋喃基]-L-脯氨酰胺
273404-37-8
VX-765(Belnacasan)
N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide VX 765
Belnacasan (VX765)
N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide
(S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide
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