Necrostatin 2 (racemate) [852391-15-2]

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Necrostatin 2 racemate (Nec-1S), the Necrostatin-1 (HY-15760) stable, is a potent and specific RIPK1 inhibitor lacking the IDO-targeting effect.

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Necrostatin 2 racemate Chemical Structure

Necrostatin 2 racemate Chemical Structure

CAS No. : 852391-15-2

This product is a controlled substance and not for sale in your territory.

Based on 14 publication(s) in Google Scholar

Other Forms of Necrostatin 2 racemate:

  • Necrostatin 2 In-stock
  • Necrostatin 2 S enantiomer In-stock

Voir tous les produits spécifiques à Isoform RIP kinase:

Voir toutes les isoformes
RIPK1 RIPK2 RIPK3
Description

Necrostatin 2 racemate (Nec-1S), the Necrostatin-1 (HY-15760) stable, is a potent and specific RIPK1 inhibitor lacking the IDO-targeting effect[1].

IC50 & Target[1]

RIPK1

 

Cellular Effect
Cell Line Type Value Description References
Jurkat IC50
206 nM
Compound: 4, 7-cl-O-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]
In Vitro

Necrostatin 2 racemate (Nec-1S) (1-100 μM; 1 h) potently inhibits RIPK1 autophosphorylation in a dose-dependent manner[1].

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

In Vivo

Necrostatin 2 racemate (Nec-1S) (6 mg/kg; i.v.; once) protects against TNF-induced systemic inflammatory response syndrome (SIRS) without sensitization effect[1].

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

Animal Model: Female C57BL/6J WT mice, SIRS model[1]
Dosage: 0.6 mg/kg or 6 mg/kg
Administration: Intravenous injection, once
Result: Showed protective effect at 6 mg/kg.
Masse moléculaire

277.71

Formule

C13H12ClN3O2

CAS No.

852391-15-2

Appearance

Solid

Color

White to light yellow

SMILES

ClC1=C2C(C(CC3C(N(C)C(N3)=O)=O)=CN2)=CC=C1

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 : ≥ 50 mg/mL (180.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6009 mL 18.0043 mL 36.0087 mL
5 mM 0.7202 mL 3.6009 mL 7.2017 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.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 3 mg/mL (10.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (10.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.65%

Références
  • [1]. Takahashi N, et al. Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models. Cell Death Dis. 2012 Nov 29;3:e437.  [Content Brief]

  • [1]. Takahashi N, et al. Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models. Cell Death Dis. 2012 Nov 29;3:e437.

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6009 mL 18.0043 mL 36.0087 mL 90.0216 mL
5 mM 0.7202 mL 3.6009 mL 7.2017 mL 18.0043 mL
10 mM 0.3601 mL 1.8004 mL 3.6009 mL 9.0022 mL
15 mM 0.2401 mL 1.2003 mL 2.4006 mL 6.0014 mL
20 mM 0.1800 mL 0.9002 mL 1.8004 mL 4.5011 mL
25 mM 0.1440 mL 0.7202 mL 1.4403 mL 3.6009 mL
30 mM 0.1200 mL 0.6001 mL 1.2003 mL 3.0007 mL
40 mM 0.0900 mL 0.4501 mL 0.9002 mL 2.2505 mL
50 mM 0.0720 mL 0.3601 mL 0.7202 mL 1.8004 mL
60 mM 0.0600 mL 0.3001 mL 0.6001 mL 1.5004 mL
80 mM 0.0450 mL 0.2251 mL 0.4501 mL 1.1253 mL
100 mM 0.0360 mL 0.1800 mL 0.3601 mL 0.9002 mL
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Necrostatin 2 racemate Related Classifications

  • Apoptosis
  • RIP kinase
Help & FAQs

Keywords:

Necrostatin 2852391-15-2Necrostatin 1S Nec-1S 7-Cl-O-Nec1Necrostatin2Necrostatin-2RIP kinaseReceptor-interacting protein kinasesRIPKNec-1stableRIPK1necroptosisIDOnecrostatinInhibitorinhibitorinhibit

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