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Qiagen 凯杰 Biosharp Omega

首页酶、辅酶及抑制剂MCE>

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Q-VD-OPh 纯度:99.26% 10mg

价:
3950.00
价:
¥3950.00

号:HY-12305

牌:MCE

账期 货到付款

(预计4-5工作日到货(以MCE官网货期为准))

工作时间

周一至周五:9:00-18:00

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0771-3293894

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客服 郭恒 蔡玉坤 曾宪飞 技术咨询

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Q-VD-OPha 是一种不可逆的泛胱天蛋白酶 (caspase) 抑制剂,具有高效的抗凋亡能力。抑制胱天蛋白酶 7 的 IC50 值别为 48 nM,抑制胱天蛋白酶 1,3,8,9,10,12 的 IC50 值在 25-400 nM 之间。Q-VD-OPha 能透过血脑屏障。

Description

Q-VD-OPha is a irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPha is able to cross the blood-brain barrier.

IC50 & Target[1]

Caspase-7

48 nM (IC50)

Caspase-3

25-400 nM (IC50)

Caspase-1

25-400 nM (IC50)

Caspase-8

25-400 nM (IC50)

Caspase-9

25-400 nM (IC50)

Caspase-10

25-400 nM (IC50)

Caspase-12

25-400 nM (IC50)

In Vitro

Q-VD-OPh is a potent inhibitor of caspase-7 with an IC50 of 48 nM utilizing a cell-free assay consisting of human recombinant caspase-7, Q-VD-OPh, and the substrate AMC-DEVD-pNa[1]. Q-VD-OPh fully inhibits caspase-3 and -7 activity at 0.05 μM. Caspase-8 is also inhibited at low Q-VD-OPh concentrations. The cleavage of PARP-1 is fully prevented at 10 μM Q-VD-OPh. DNA fragmentation and disruption of the cell membrane functionality are both prevented at 2 μM Q-VD-OPh[2]. Q-VD-OPh is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk, and is also equally effective in preventing apoptosis mediated by the three major apoptotic pathways, caspase 9/3, caspase 8/10, and caspase12. Q-VD-OPh is not toxic to cells even at extremely high concentrations[3]. QVD is also able to increase the expression of differentiation markers in acute myeloid leukemia (AmL) blasts. QVD alone or combined with VDDs increases differentiation and HPK1-cJun signaling in AmL cell context-dependent manner[4].

In Vivo

Chronic treatment with Q-VD-OPh prevents caspase-7 activation and limits the pathological changes associated with tau, including caspase cleavage. Q-VD-OPh could be a potential therapeutic compound for the treatment of Alzheimer's disease[1].

Solvent & Solubility
In Vitro:  

DMSO : ≥ 25 mg/mL (48.69 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9475 mL 9.7373 mL 19.4746 mL
5 mM 0.3895 mL 1.9475 mL 3.8949 mL
10 mM 0.1947 mL 0.9737 mL 1.9475 mL
* Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mouse: Stock solutions of Q-VD-OPh are prepared in DMSO and diluted in sterile PBS solution prior to injection. A final concentration of 10 mg/kg is chosen indicating neuroprotection at this concentration of Q-VD-OPh. Three-month old mice are divided into two groups: control, vehicle (n=3) or treated (n=2). Mice are injected i.p. three times a week with either Q-VD-OPh or vehicle for a total time period of 3 months[1].

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

References
Molecular Weight

513.49

Formula

C₂₆H₂₅F₂N₃O₆

CAS No.

1135695-98-5

SMILES

O=C(O)C[C@H](NC([C@@H](NC(C1=NC2=CC=CC=C2C=C1)=O)C(C)C)=O)C(COC3=C(F)C=CC=C3F)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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