M5049
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $1350 | Check With Us |
| 200mg | $2025 | Check With Us |
| 500mg | $3415 | Check With Us |
: Cat #: V3364 CAS #: 2101938-42-3 Purity ≥ 99%
Description: Enpatoran (M-5049) is a novel and selective inhibitor of Toll-Like Receptor 7/8 with IC50 of 11.1 and 24 nM, respectively.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 320.31 |
|---|---|
| Molecular Formula | C16H15F3N4 |
| CAS No. | 2101938-42-3 |
| SMILES Code | N[C@]1([H])C[C@]([H])(C(F)(F)F)CN(C2=CC=C(C#N)C3=C2C=CC=N3)C1 |
| Synonyms | Enpatoran; M 5049; M5049; M-5049; |
| Protocol | In Vitro | Enpatoran (0.01 nM-10 μM) inhibits production of IL-6 stimulated by all the ligands (miR-122, Let7c RNA, Alu RNA, and R848) with IC50 values ranging from 35 to 45 nM. |
|---|---|---|
| In Vivo | Enpatoran exhibits moderate half-lives (mouse 1.4, rat 5.0 and dog 13 h) due to high plasma clearance (1.4, 1.2 and 0.59 L/h/kg, respectively) combined with large volumes of distribution (2.7, 8.7 and 5.7 L/kg, respectively) following intravenous administration (mouse, rat and dog 1.0 mg/kg). Enpatoran (M5049) exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg). Pre-treatment with Enpatoran (M5049; oral gavage; 1 mg/kg) before R848 (intraperitoneal injection of 25 µg) dose-dependently inhibits the production of IL-6 and IFN-α in mice. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.1220 mL | 15.6099 mL | 31.2198 mL | 62.4395 mL |
| 5mM | 0.6244 mL | 3.1220 mL | 6.2440 mL | 12.4879 mL |
| 10mM | 0.3122 mL | 1.5610 mL | 3.1220 mL | 6.2440 mL |
| 20mM | 0.1561 mL | 0.7805 mL | 1.5610 mL | 3.1220 mL |
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.