VX-765 | CAS# 273404-37-8 APExBIO 貨號A8238
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雷帕黴菌(Rapamycin)| Romidepsin (FK228, depsipeptide) | Daptomycin | G-418 (80 S 核醣體延伸抑制劑)
Proteases系列產品
蛋白酶(Proteases)也稱為肽酶(peptidases)或蛋白水解酶(proteolytic enzymes),由大量催化肽鍵水解(hydrolysis)並隨後導致蛋白質底物(protein substrates)降解為氨基酸(amino acids)的酶組成。蛋白酶(Proteases)與多種人類疾病有關,包括癌症(cancer)、神經退行性疾病(neurodegenerative disorders)、炎症性疾病(inflammatory diseases)和心血管疾病(cardiovascular diseases)。因此,許多蛋白酶抑制劑【小分子(small molecules)和蛋白質】已被鑑定為阻斷蛋白酶的活性(proteases)。蛋白酶抑制劑可以根據它們通過兩種一般機制抑制的蛋白酶類別分為不同的類型,即不可逆的“捕獲(trapping)”反應和可逆(reversible)的緊密結合反應。蛋白酶抑制劑已被用作治療蛋白酶相關疾病的診斷劑(diagnostic)或治療劑(therapeutic agents)。
VX-765 | CAS# 273404-37-8 APExBIO 貨號A8238
Product Citation+4
Caspase-1 inhibitor,potent and selective
VX-765 是 VRT-043198 的口服吸收前藥(orally- absorbed pro-drug),是一種有效的選擇性 caspase-1 抑制劑,屬於 ICE/caspase-1 亞家族 caspase。Caspase-1 被稱為白細胞介素 (interleukin , IL)-1 轉換酶,負責將關鍵炎症介質 IL-1β (inflammatory mediator IL-1β)從無活性前體加工成有活性的分泌蛋白。據報導,作為對細胞內細菌的反應,caspase-1 參與了一個快速的細胞死亡程序(programme of cell death),稱為巨噬細胞(macrophages)中的細胞焦亡(pyroptosis )[1]。
VX-765 通常代謝為活性分子 VRT-043198。在用細菌產物刺激的外周血單個核細胞培養物中,VRT-043198 抑制白細胞介素 (IL)-1β 和 IL-18 的釋放,但不影響其他細胞因子如 IL-α、TNFα、IL-6 的分泌和 IL-8 [2]。該產品也用於其他模型以說明 Caspase-1 的功能。口服 VX-765 可顯著降低類風濕關節炎(rheumatoid arthritis)和皮膚炎症(skin inflammation)小鼠模型的疾病嚴重程度以及炎性細胞因子(inflammatory cytokines)和趨化因子(chemokines)的分泌[1]。此外,最近的研究表明,VX-765 在 HIV 感染的淋巴組織(HIV-infected lymphoid tissues)中以劑量依賴性方式預防 CD4 T 細胞焦亡死亡(T-cell pyroptotic death) [3]。
- Hila Israelov, Orly Ravid, et al. “Caspase-1 has a critical role in blood-brain barrier injury and its inhibition contributes to multifaceted repair.” J Neuroinflammation 2020 Sep 9;17(1):267.PMID:32907600
- Darren C. Johnson, Marian C. Okondo, et al. “DPP8/9 inhibitors activate the CARD8 inflammasome in resting lymphocytes.” Cell Death Dis. 2020 Aug 14;11(8):628.PMID:32796818
- Panina SB, Baran N, et al. “A mechanism for increased sensitivity of acute myeloid leukemia to mitotoxic drugs.” Cell Death Dis. 2019 Aug 13;10(8):617.PMID:31409768
- Yang G, Wang J, et al. “White spot syndrome virus infection activates Caspase 1-mediated cell death in crustacean.” Virology. 2018 Dec 13;528:37-47.PMID:30554072
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 508.99 |
Cas No. | 273404-37-8 |
Formula | C24H33ClN4O6 |
Solubility | insoluble in H2O; ≥313 mg/mL in DMSO; ≥50.5 mg/mL in EtOH with ultrasonic |
Chemical Name | (2S)-1-[(2S)-2-[(4-amino-3-chlorobenzoyl)amino]-3,3-dimethylbutanoyl]-N-[(2R,3S)-2-ethoxy-5-oxooxolan-3-yl]pyrrolidine-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | CCOC1C(CC(=O)O1)NC(=O)C2CCCN2C(=O)C(C(C)(C)C)NC(=O)C3=CC(=C(C=C3)N)Cl |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
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VX-765 | CAS# 273404-37-8 | 貨號A8238 | Caspase-1 inhibitor |
APExBIO提供優質的胜肽和生物分析試劑,廣泛產品線如Protease、Chromatin/Epigenetics表觀遺傳學、MAPK Signal、DNA Damege/DNA repair、細胞凋亡、腫瘤生物學、Stem cell等研究領域, 還提供定制的服務,包括多肽合成,抗體的生產和檢測的發展。產品線DNA/RNA prep kit、Drug Screening panel、Bioactive peptides、Growth factors、Biotinylation Reagents、tag peptides、amino Acids、Growth factors等。APExBIO產品質量都伴隨著證書的分析,高效液相色譜,質譜,和HMNR數據。
A5932 | Candesartan | 139481-59-7 | 99.01% | Angiotensin II receptor 1 (AT1) antagonist |
A5970 | Irbesartan | 138402-11-6 | 99.52% | Angiotensin II inhibitor |
A5979 | Tie2 kinase inhibitor | 948557-43-5 | 99.88% | Tie-2(Tie2 ) inhibitor |
A6001 | 3X (DYKDDDDK) Peptide | 402750-12-3 | 98.66% | Synthetic peptide tag |
A6002 | DYKDDDDK tag Peptide | 98849-88-8 | 98.08% | Versatile fusion tag |
A6003 | c-Myc tag Peptide | 98.08% | Synthetic peptide tag | |
A6004 | Influenza Hemagglutinin (HA) Peptide | 92000-76-5 | 99.22% | Epitope of HA tag peptide |
A6005 | V5 Epitope Tag Peptide | 99.67% | Peptide sequence-GKPIPNPLLGLDST | |
A6006 | Hexa His tag peptide | 99.90% | Synthetic 6XHis peptide | |
A6007 | S Tag Peptide | 96.56% | Pancreatic RNase A derivtive | |
A6008 | T7 Tag Peptide | 99.99% | Peptide sequence-MASMTGGQQMG | |
A6009 | VSV-G Peptide | 99.99% | Peptide sequence-YTDIEMNRLGK | |
A6010 | X-press Tag Peptide | 99.23% | Petide sequence-DLYDDDDK | |
A6100 | Fmoc-L-Arg(Aloc)2-OH | 148893-34-9 | 99.65% | |
A6576 | Rink Amide Resin | 13653-84-4 | 98.00% | SPS of peptide amides |