1. Anti-infection Apoptosis NF-κB
  2. HIV IAP NF-κB
  3. Ciapavir

Ciapavir (SBI-0953294) 是一种 HIV-1 潜伏逆转剂,可在体外和体内逆转潜伏的 HIV-1 储库,且不会引起系统性 T 细胞活化或广泛的细胞因子释放。Ciapavir 能降解 cIAP1 并激活非经典 NF-κB 通路。Ciapavir 可用于 HIV-1 感染的研究。

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Ciapavir

Ciapavir Chemical Structure

CAS No. : 2433895-70-4

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  • 生物活性

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  • 参考文献

生物活性

Ciapavir (SBI-0953294) is a HIV-1 latency-reversing agent. Ciapavir reverses latent HIV-1 reservoir in vitro and in vivo without inducing systemic T cell activation or broad cytokine release. Ciapavir degrades cIAP1 and activates non-canonical NF-κB pathway. Ciapavir can be used for the research of HIV-1 infection[1].

IC50 & Target[1]

HIV-1

 

cIAP

 

体外研究
(In Vitro)

Ciapavir (0.1-10000 nM;作用 48 小时) 通过激活非经典 NF-κB 通路介导 2D10 Jurkat 细胞中 HIV-1 的潜伏期逆转[1]
Ciapavir (1-10 μM;作用 24 h) 在浓度高达 10 μM 时,不会在人外周血单个核细胞 (PBMCs) 或静息 CD4+ T 细胞中触发细胞因子释放或 T 细胞活化[1]
Ciapavir (0.1-10000 nM;作用 48 小时) 可与 BET 抑制剂 JQ1 (HY-13030) 和 I-BET151 (HY-13235) 产生协同作用,增强 2D10 Jurkat 细胞中 HIV-1 的潜伏期逆转[1]

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

体内研究
(In Vivo)

Ciapavir (10-20 mg/kg;腹腔注射;单剂量) 在 C57BL/6J 小鼠中表现出强烈的靶点结合 (cIAP1 降解) 作用,且不会引发显著的细胞因子释放[1]
Ciapavir (10-20 mg/kg;腹腔注射;单剂量) 可在接受抗逆转录病毒疗法治疗的 BLT 小鼠中诱导潜伏 HIV-1 表达,且无明显免疫激活[1]

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

Animal Model: B6.129S-Rag2tm1Fwa Cd47tm1Fpl Il2rgtm1Wjl/J (male and female, 3 months old)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: I.p., single dose
Result: Caused three of nine treated mice to exhibit increases in plasma HIV RNA 48 hours post-administration.
caused four of six mice in the 20 mg/kg group to show a significant increase in bone marrow HIV RNA.
Did not cause significant upregulation of CD69 in blood CD45+ cells or CD4+ T cells, or in bone marrow CD45+ cells.
Induced modest CD69 upregulation in bone marrow CD4+ T cells at 10 mg/kg but not 20 mg/kg.
分子量

1023.31

Formula

C54H70N8O8S2

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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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • 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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Ciapavir
目录号:
HY-134844
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