Ac-YVAD-CHO(Synonyms: L-709049)

Ac-YVAD-CHO;(Synonyms: L-709049)

Ac-YVAD-CHO (L-709049) 是一种有效的、可逆的、特异性的四肽白介素 1β 转化酶 (ICE) 抑制剂,小鼠和人类 Ki 值分别为 3.0 和 0.76 nM。Ac-YVAD-CHO 可抑制成熟 IL-lβ 的产生。

Ac-YVAD-CHOamp;;(Synonyms: L-709049)

Ac-YVAD-CHO Chemical Structure

CAS No. : 143313-51-3

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生物活性

Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO can suppress the production of mature IL-lβ[1].

IC50 Target

IL-1β

3 nM (Ki)

IL-1β

0.76 nM (Ki)

体外研究
(In Vitro)

Ac-YVAD-CHO inhibits IL-1β in a dose-dependent manner, with mouse and human IC50 values of 2.5 and 0.7 μM. Ac-YVAD-CHO (0.01~100 μM) reduces the elevations of IL-lβ in the plasma and peritoneal fluid treated with LPS in a dose-related manner[1].

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

体内研究
(In Vivo)

Ac-YVAD-CHO (10 mg/kg; i.p.; 1 hour) is absorbed from the peritoneal cavity, as well as cleared from the blood rapidly[1].
Ac-YVAD-CHO (50 mg/kg; i.p.; 1 hour) drops precipitously to approximately 1 and 0.2 μM at 30 and 60 minutes after injection[1].
Ac-YVAD-CHO (30 mg/kg; i.p.; 6 hours) suppresses IL-1β levels[1].

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

Animal Model: CD1 female mice
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: I.p.; 1 hour
Result: Absorbed from the peritoneal cavity, as well as cleared from the blood rapidly.
Animal Model: CD1 female mice
Dosage: 50 mg/kg (Pharmacokinetic Analysis)
Administration: I.p.; 1 hour
Result: Dropped precipitously to approximately 1 and 0.2 μM at 30 and 60 minutes after injection.
Animal Model: P. acnes-sensitized mice
Dosage: 30 mg/kg
Administration: I.p.; 6 hours
Result: Suppressed IL-1β levels.

分子量

492.52

Formula

C23H32N4O8

CAS 号

143313-51-3

Sequence Shortening

Ac-YVAD-CHO

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.

参考文献
  • [1]. Fletcher DS, et al. A synthetic inhibitor of interleukin-1 beta converting enzyme prevents endotoxin-induced interleukin-1 beta production in vitro and in vivo. J Interferon Cytokine Res. 1995;15(3):243-248.

Z-YVAD-FMK

Z-YVAD-FMK; 纯度: ge;98.0%

Z-YVAD-FMK 是一种具有细胞通透性 caspase-1caspase-4 抑制剂,具有抗炎和抗肿瘤活性。

Z-YVAD-FMKamp;;

Z-YVAD-FMK Chemical Structure

CAS No. : 210344-97-1

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ¥6940 In-stock
1 mg ¥2200 In-stock
5 mg ¥5000 In-stock
10 mg ¥8200 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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Z-YVAD-FMK 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Z-YVAD-FMK is a cell-permeable caspase-1 and -4 inhibitor with anti-inflammatory and anti-tumor activities[1].

IC50 Target

Caspase

;

体外研究
(In Vitro)

Z-YVAD-FMK (100 μM; 24 hours) significantly downregulated the growth inhibition induced by butyrate in Caco-2 cells[1].
Z-YVAD-FMK (20 μM; pre 1 hour; 24 hours) attenuates the apoptotic induction of III-10 on both HepG2 and BEL-7402 cells, the apoptotic rate of -10 on HepG2 cells is reduced by Z-VAD-FMK from 19.88% to 8.34%, while that on BEL-7402 cells is reduced from 17.56% to 11.98%[4].

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

Cell Viability Assay[1]

Cell Line: Caco-2 cells
Concentration: 0-100 μM
Incubation Time: 24 hours
Result: Inhibited Caco-2 cells growth.

Apoptosis Analysis[1]

Cell Line: BEL-7402 and HepG2 cells
Concentration: 20 μM
Incubation Time: Pre 1 hour; 24 hours
Result: Induced a caspase-dependent apoptosis in cells.

分子量

630.66

Formula

C31H39FN4O9

CAS 号

210344-97-1

Sequence

Z-Tyr-Val-Ala-Asp-FMK

Sequence Shortening

Z-YVAD-FMK

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 125 mg/mL (198.21 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5856 mL 7.9282 mL 15.8564 mL
5 mM 0.3171 mL 1.5856 mL 3.1713 mL
10 mM 0.1586 mL 0.7928 mL 1.5856 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.30 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.30 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.30 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Li H1,et al.Aluminum hydroxide adjuvants activate caspase-1 and induce IL-1beta and IL-18 release.J Immunol. 2007 Apr 15;178(8):5271-6.

    [2]. Avivi-Green C, et al. Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines.J Nutr. 2002 Jul;132(7):1812-8.