1. Apoptosis NF-κB
  2. Necroptosis RANKL/RANK
  3. Necrostatin-7

Necrostatin-7 (Nec-7) is a Necroptosis inhibitor with an EC50 of 10.6 μM. Necrostatin-7 inhibits signal transduction from RANK to NFATc1 without affecting the activation of MAPK or NF-κB. Necrostatin-7 suppresses the expression levels of Acp5, Atp6v0d2, Ctsk and Dcstamp. Necrostatin-7 reduces myocardial infarction size, ameliorates adverse left ventricular remodeling, decreases myocardial wall stress, reduces the amount and length of scar tissue, and improves left ventricular function. Necrostatin-7 exerts cardioprotective effects in a rat model of permanent coronary artery occlusion. Necrostatin-7 can be used in research related to osteolytic bone diseases and myocardial infarction.

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Necrostatin-7

Necrostatin-7 Chemical Structure

CAS No. : 351062-08-3

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Description

Necrostatin-7 (Nec-7) is a Necroptosis inhibitor with an EC50 of 10.6 μM. Necrostatin-7 inhibits signal transduction from RANK to NFATc1 without affecting the activation of MAPK or NF-κB. Necrostatin-7 suppresses the expression levels of Acp5, Atp6v0d2, Ctsk and Dcstamp. Necrostatin-7 reduces myocardial infarction size, ameliorates adverse left ventricular remodeling, decreases myocardial wall stress, reduces the amount and length of scar tissue, and improves left ventricular function. Necrostatin-7 exerts cardioprotective effects in a rat model of permanent coronary artery occlusion. Necrostatin-7 can be used in research related to osteolytic bone diseases and myocardial infarction[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
Jurkat EC50
10.6 μM
Compound: nec-7
Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat cells
Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat cells
[PMID: 18768316]
In Vitro

Necrostatin-7 (0.1-3 μM; 3 days) dose-dependently inhibits M-CSF- and RANKL-induced osteoclast differentiation in primary bone marrow-derived macrophages at concentrations from 0.1 to 3 μM, with near-complete inhibition at 2 μM and 3 μM, without reducing BMM viability[1].
Necrostatin-7 (1-3 μM; 5 days) dose-dependently inhibits osteoclastic bone resorption by primary bone marrow-derived macrophages at concentrations from 1 to 3 μM, with near-complete inhibition at 2 μM and 3 μM after 5 days of treatment[1].
Necrostatin-7 (1-3 μM; 1-3 days) dose-dependently suppresses RANKL-induced expression of osteoclastogenic marker genes (Acp5, Atp6v0d2, Ctsk, Dcstamp) in primary bone marrow-derived macrophages at 1 μM and 3 μM over 1 to 3 days of differentiation[1].
Necrostatin-7 (1-3 μM; 1-3 days) dose-dependently inhibits RANKL-induced NFATc1 autoamplification in primary bone marrow-derived macrophages at 1 μM and 3 μM over 1 to 3 days of differentiation, with near-complete suppression at 3 μM[1].
Necrostatin-7 inhibits TNF-α-induced necroptosis in FADD-deficient human Jurkat T cells with an EC50 of 10.6 μM[2].

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

In Vivo

Necrostatin-7 (14.5 mg/kg; i.p.; single dose 1 hour prior to permanent coronary occlusion) exerts cardioprotective properties, reducing myocardial wall stress (evidenced by lower NT-proBNP levels) and myocardial remodeling (evidenced by 9.0% infarct size) in rats with permanent coronary occlusion-induced myocardial infarction[3].
Pretreatment with necrostatin-7 (14.5 mg/kg; i.p.) reduces left ventricular scar tissue and scar length, and lowers plasma N-terminal pro-brain natriuretic peptide levels, indicating improved left ventricular function in rats with permanent coronary occlusion-induced myocardial infarction[4].

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

Animal Model: Wistar rats (male)[3]
Dosage: 14.5 mg/kg
Administration: i.p.; single dose 1 hour prior to permanent coronary occlusion
Result: Reduced serum NT-proBNP level to 0.2 ng/mL.
Reduced myocardial infarct size to 9.0%.
Reduced infarct length to 2.9 mm.
Animal Model: strain not specified[4]
Dosage: 14.5 mg/kg
Administration: i.p.; single dose 60 minutes before coronary occlusion
Result: Reduced the amount of scar tissue and scar length in the left ventricle.
Decreased plasma levels of N-terminal pro-brain natriuretic peptide.
Molecular Weight

371.41

Formula

C16H10FN5OS2

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C1N(C2=NC=CS2)C(S/C1=C\C3=CNN=C3C4=CC=C(F)C=C4)=N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (26.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6924 mL 13.4622 mL 26.9244 mL
5 mM 0.5385 mL 2.6924 mL 5.3849 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.64%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6924 mL 13.4622 mL 26.9244 mL 67.3111 mL
5 mM 0.5385 mL 2.6924 mL 5.3849 mL 13.4622 mL
10 mM 0.2692 mL 1.3462 mL 2.6924 mL 6.7311 mL
15 mM 0.1795 mL 0.8975 mL 1.7950 mL 4.4874 mL
20 mM 0.1346 mL 0.6731 mL 1.3462 mL 3.3656 mL
25 mM 0.1077 mL 0.5385 mL 1.0770 mL 2.6924 mL
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  • 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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Necrostatin-7
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