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Peficitinib (ASP-015K, JNJ-54781532)

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Peficitinib (ASP-015K, JNJ-54781532)
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250mg$1150Check With Us
500mg$1750Check With Us
1g$2625Check With Us

Cat #: V0321 CAS #: 944118-01-8 Purity ≥ 98%

Description: Peficitinib (formerly ASP015K and JNJ54781532) is a novel, potent and orally bioavailable inhibitor of Janus kinase-JAK with potential anti-inflammatory activities.

References: Ito M, et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33.

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Molecular Weight (MW)326.39
Molecular FormulaC18H22N4O2
CAS No.944118-01-8
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 65 mg/mL (199.1 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In VivoChemical Name: 4-(((1R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl)amino)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide SMILES Code: O=C(C1=CN=C(NC=C2)C2=C1N[C@H]3[C@]4([H])C[C@@]5([H])C[C@](C4)(O)C[C@]3([H])C5)N
SynonymsJNJ54781532; JNJ54781532; JNJ 54781532; ASP015K; ASP015K; ASP 015K; Peficitinib;
ProtocolIn VitroPeficitinib hydrobromide (10-1000 nM) inhibits IL-2-induced STAT5 phosphorylation in a concentration-dependent manner with a mean IC50 of 124 nM in rat whole blood, and inhibits STAT5 phosphorylation with a mean IC50 of 127 nM in human lymphocytes. Peficitinib hydrobromide (0-100 nM; 3 days) inhibits IL-2-induced T cell proliferation in a concentration-dependent manner.
In VivoPeficitinib hydrobromide (1-30 mg/kg; p.o.; once daily for 24 days) shows dose-dependent efficacy both in prophylactic and therapeutic dosing regimens in an adjuvant-induced arthritis rat model.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM3.0638 mL15.3191 mL30.6382 mL61.2764 mL
5mM0.6128 mL3.0638 mL6.1276 mL12.2553 mL
10mM0.3064 mL1.5319 mL3.0638 mL6.1276 mL
20mM0.1532 mL0.7660 mL1.5319 mL3.0638 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.