pt en es

Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Necrostatin-1 [4311-88-0]

Imprimir

Referência HY-15760-1mL

Tamanho : 10mM/1mL

Contactar o distribuidor local :

Telefone : +1 850 650 7790

Marca : MedChemExpress

Solicitar mais informações

Contactar o distribuidor local :

Telefone : +1 850 650 7790

Description

Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC₅₀ of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC₅₀=182 nM). Necrostatin-1 is also an IDO inhibitor^[1].

IC₅₀ & Target

EC50: 182 nM (RIP1 kinase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	CC₅₀	> 50 μM Compound: 1	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by celltiter glo assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by celltiter glo assay	[PMID: 37494773]
HT-29	EC₅₀	> 10 μM Compound: Nec-1	Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 4 hrs followed by fresh medium replacement without compound by CCK8 assay Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 4 hrs followed by fresh medium replacement without compound by CCK8 assay	[PMID: 39180479]
Jurkat	EC₅₀	0.05 μM Compound: (+/-)-1	Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat T cells Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat T cells	[PMID: 18467094]
Jurkat	EC₅₀	0.49 μM Compound: 1	Effective concentration required for inhibition of necroptosis in FADD deficient Jurkat T cells treated with TNF-alpha Effective concentration required for inhibition of necroptosis in FADD deficient Jurkat T cells treated with TNF-alpha	[PMID: 16153840]
Jurkat	EC₅₀	0.49 μM Compound: Nec-1	Anti-necroptic activity in TNFalpha-induced human Jurkat cells assessed as cell viability pretreated for 24 hrs followed by TNFalpha induction by Cell-titer-glo assay Anti-necroptic activity in TNFalpha-induced human Jurkat cells assessed as cell viability pretreated for 24 hrs followed by TNFalpha induction by Cell-titer-glo assay	[PMID: 36724216]
Jurkat	EC₅₀	0.54 μM Compound: Nec-1	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability by MTT assay	[PMID: 38199165]
Jurkat	EC₅₀	182 nM Compound: 1	Inhibition of endogenous RIP1 autophosphorylation in human Jurkat cells Inhibition of endogenous RIP1 autophosphorylation in human Jurkat cells	[PMID: 18408713]
Jurkat	EC₅₀	490 nM Compound: 1	Inhibition of cellular necroptosis in TNFalpha treated FADD deficient human Jurkat cells Inhibition of cellular necroptosis in TNFalpha treated FADD deficient human Jurkat cells	[PMID: 18408713]
Jurkat	IC₅₀	494 nM Compound: 1, Nec-1	Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cell deficient in FADD assessed as cell viability after 30 hrs by ATP based viability assay in presence of TNFalpha Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cell deficient in FADD assessed as cell viability after 30 hrs by ATP based viability assay in presence of TNFalpha	[PMID: 16408008]
Sf9	IC₅₀	182 nM Compound: Necrostatin-1	Inhibition of recombinant human GST-fused RIPK1 (1 to 497 residues) expressed in baculovirus infected insect Sf9 cells in presence of 32P-gamma-ATP after 30 mins by autoradiogram-based Western blot method Inhibition of recombinant human GST-fused RIPK1 (1 to 497 residues) expressed in baculovirus infected insect Sf9 cells in presence of 32P-gamma-ATP after 30 mins by autoradiogram-based Western blot method	[PMID: 28280261]

In Vitro

Necrostatin-1 (Nec-1) efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors^[1].
Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI)^[2].
Necrostatin-1 (Nec-1) (30 μM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death^[4].

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

In Vivo

Necrostatin-1 (Nec-1) induces tubular bilation and affects the kinetics of the dilation of peritubular capillaries after RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kg body weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observation period^[2].

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

Masse moléculaire

259.33

Formule

C₁₃H₁₃N₃OS

CAS No.

4311-88-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(CC1=CNC2=C1C=CC=C2)N3)N(C)C3=S

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (482.01 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	3.8561 mL	19.2805 mL	38.5609 mL
5 mM	0.7712 mL	3.8561 mL	7.7122 mL
10 mM	0.3856 mL	1.9280 mL	3.8561 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% (50% EtOH 50% Cremophor EL) 90% Saline
Solubility: 1.67 mg/mL (6.44 mM); Suspended solution; Need ultrasonic

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 12.5 mg/mL (48.20 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.89%

Fiche technique (283 KB) SDS (393 KB)

COA (254 KB) RP-HPLC (242 KB) Elemental Analysis Report (112 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9. [Content Brief]

[2]. Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57. [Content Brief]

[3]. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326. [Content Brief]

[4]. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91. [Content Brief]

[5]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124. [Content Brief]

Você também pode estar interessado nos seguintes produtos:

Referência

Descrição

Cond.

Price Bef. VAT

HY-16082-1mL

AZD7545 [252017-04-2]

10mM/1mL

HY-100573-1mL

Necrosulfonamide [1360614-48-7]

10mM/1mL

Necrostatin-1 [4311-88-0]

Referência HY-15760-1mL

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

Necrostatin-1 Related Antibodies

Você também pode estar interessado nos seguintes produtos: