[CAS NO. 915363-56-3]  Cotinhibitor-2

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PRODUCTS SPECIFICATIONS [915363-56-3]

Catalog
HY-32018
Brand
MCE
CAS
915363-56-3

DESCRIPTION [915363-56-3]

Overview

MDLMFCD13184702
Molecular Weight539.43
Molecular FormulaC26H25Cl2FN8
SMILESN#CC1=C(C2=CC(NCC3=CN(N=N3)C4CCN(CC4)CC)=CC(Cl)=C2N=C1)NC5=CC=C(F)C(Cl)=C5

For research use only. We do not sell to patients.


Summary

Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC 50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC 50 of 0.3 μM [1] .


IC50 & Target

COT/Tpl2 [1]


In Vivo

Cot inhibitor-2 (compound 34) is orally administered in rats with 100 mg/kg dosing and showed a C max of 517 ng/mL (0.89 μM) and AUC of 4841 ng•h/mL. Cot inhibitor-2 is tested in the LPS-induced TNF-α production model in female Sprague-Dawley rats. With a 25 mg/kg po dose, Cot inhibitor-2 inhibits LPS-induced TNF-α production by 83% [1] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

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

Solvent & Solubility

In Vitro:

DMSO : 40 mg/mL ( 74.15 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8538 mL 9.2690 mL 18.5381 mL
5 mM 0.3708 mL 1.8538 mL 3.7076 mL
10 mM 0.1854 mL 0.9269 mL 1.8538 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 3 mg/mL (5.56 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 3 mg/mL (5.56 mM); Clear solution

  • 3.

    Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

    Solubility: ≥ 2 mg/mL (3.71 mM); Clear solution

* All of the co-solvents are available by MCE.