Necrostatin-5

Names

[ Name ]:
Necrostatin-5

[Synonym ]:
{[3-(4-Methoxyphenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl}acetonitrile
Acetonitrile, 2-[[3,4,5,6,7,8-hexahydro-3-(4-methoxyphenyl)-4-oxo[1]benzothieno[2,3-d]pyrimidin-2-yl]thio]-
Necrostatin-5
Nec-5

Biological Activity

[Description]:

Necrostatin-5 (Nec-5) is a potent necroptosis inhibitor with an EC50 value of 0.24 µM. Necrostatin-5 also is a RIP1 inhibitor. Necrostatin-5 shows cardioprotective effects[1][2][3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> RIP kinase

Research Areas >> Neurological Disease

[Target]

RIPK1

necroptosis:0.24 μM (EC50)

[In Vitro]

Necrostatin-5 (1、5、10、50、100 µM) 以剂量依赖性方式抑制 LDH 释放[3]。 Necrostatin-5 (100 µM) 保护 MH-S 细胞免受 S. aureus, Listeria monocytogenes, S. pneumoniae, uropathogenic Escherichia coli (UPEC) 的攻击，并防止肺炎球菌溶血素引起的死亡[3]。

[In Vivo]

Necrostatin-5 (2.46 mg/kg；腹腔注射) 对大鼠离体心脏模型显示心脏保护作用[2]。 Animal Model: 200-300 g, male Wistar rats[2] Dosage: 2.46 mg/kg Administration: I.p.; 60 min before experiment Result: Reduced the infarction zone caused by 30-min global ischemia and 120-min reperfusion.

[References]

[1]. Wang K, et al. Structure-activity relationship analysis of a novel necroptosis inhibitor, Necrostatin-5. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1455-65.

[2]. Dmitriev YV, et al. Study of cardioprotective effects of necroptosis inhibitors on isolated rat heart subjected to global ischemia-reperfusion. Bull Exp Biol Med. 2013 Jun;155(2):245-8.

[3]. González-Juarbe N, et al. Pore-Forming Toxins Induce Macrophage Necroptosis during Acute Bacterial Pneumonia. PLoS Pathog. 2015 Dec 11;11(12):e1005337.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
640.4±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₇N₃O₂S₂

[ Molecular Weight ]:
383.49

[ Flash Point ]:
341.1±34.3 °C

[ Exact Mass ]:
383.076202

[ PSA ]:
121.45000

[ LogP ]:
4.01

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.724

[ Storage condition ]:
-20°C

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H319-H413

[ Precautionary Statements ]:
P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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