[CAS NO. 1006378-90-0]  p38MAPK-IN-1

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PRODUCTS SPECIFICATIONS [1006378-90-0]

Distributor
Catalog
AS906027
Brand
Arctom Scientific
CAS
1006378-90-0

DESCRIPTION [1006378-90-0]

Overview

MDLMFCD28900744
Molecular Weight349.35
Molecular FormulaC21H15F2N2O
SMILESFC1=CC(F)=C(C2=CC=NC(C2=CC=[NH+]3[O-])=C3C4=C(C)C=CC=C4)C=C1

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


Summary

p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC 50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.


IC50 & Target

p38 MAPK

68 nM (IC 50 )


In Vivo

p38 MAPK-IN-1 (Compound 4; 1 mg/kg for iv and 10 mg/kg for po) has a t 1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a C max of 5.3 μM for po in male wistar rats [1] .
p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED 50 of 0.5 mg/kg [1] .

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

Animal Model: Male wistar rats [1]
Dosage: 10 mg/kg for po and 1 mg/kg for iv (Pharmacokinetic Analysis)
Administration: Po and iv
Result: Had a t 1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a C max of 5.3 μM for po.

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 : 33.33 mg/mL ( 95.41 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8625 mL 14.3123 mL 28.6246 mL
5 mM 0.5725 mL 2.8625 mL 5.7249 mL
10 mM 0.2862 mL 1.4312 mL 2.8625 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: ≥ 0.83 mg/mL (2.38 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.83 mg/mL (2.38 mM); Clear solution

  • 3.

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

    Solubility: ≥ 0.83 mg/mL (2.38 mM); Clear solution

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