ChemicalBook >> CAS DataBase List >>8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]-

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]-

CAS No.
2101938-42-3
Chemical Name:
8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]-
Synonyms
Enpatoran;M5049;Enpatoran/ M5049;Enpatoran, 10 mM in DMSO;5-[(3R,5S)-3-Amino-5-(trifluoromethyl)-1-piperidyl]quinoline-8-carbonitrile;5-((3R,5S)-3-Amino-5-(trifluoromethyl)piperidin-1-yl)quinoline-8-carbonitrile;8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]-;inhibit,M5049,Inhibitor,Toll-like Receptor (TLR),M-5049,autoimmunity,M 5049,TLR7/8,selective,Enpatoran
CBNumber:
CB18344428
Molecular Formula:
C16H15F3N4
Molecular Weight:
320.31
MDL Number:
MFCD34471096
MOL File:
2101938-42-3.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-07-20 17:44:43
Product description Number Pack Size Price
Enpatoran BJD93842 1mg $389.4
Enpatoran BJD93842 2mg $649
Enpatoran BJD93842 5mg $1038.4
Enpatoran BJD93842 10mg $1557.6
Enpatoran BJD93842 25mg $2596

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- Properties

Boiling point 477.8±45.0 °C(Predicted)
Density 1.37±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : 24.44 mg/mL (76.30 mM; Need ultrasonic)
pka 9.50±0.40(Predicted)
form Solid
color Light yellow to yellow
FDA UNII 7CZ390V26X

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Biosynth BJD93842 Enpatoran 2101938-42-3 1mg $389.4 2026-06-04 Buy
Biosynth BJD93842 Enpatoran 2101938-42-3 2mg $649 2026-06-04 Buy
Biosynth BJD93842 Enpatoran 2101938-42-3 5mg $1038.4 2026-06-04 Buy
Biosynth BJD93842 Enpatoran 2101938-42-3 10mg $1557.6 2026-06-04 Buy
Biosynth BJD93842 Enpatoran 2101938-42-3 25mg $2596 2026-06-04 Buy
Product number Packaging Price Buy
BJD93842 1mg $389.4 Buy
BJD93842 2mg $649 Buy
BJD93842 5mg $1038.4 Buy
BJD93842 10mg $1557.6 Buy
BJD93842 25mg $2596 Buy

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- Chemical Properties,Uses,Production

Uses

Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research [1].

in vivo

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[1].
Enpatoran (M5049) exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg)[1].
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)[1].

Animal Model:Female C57BL/6 mice[1]
Dosage:0.1 mg/kg and 1 mg/kg
Administration:Oral gavage; administered 1 hour prior to R848 challenge
Result:The TLR7/8 agonist R848 stimulated both IFN-α and IL-6 production in mice.
Enpatoran decreased IFN-α and IL-6 production stimulated by R848.
Animal Model:Female CD1 mice, Female Wistar rats, Female beagle dogs[1]
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:Intravenous (i.v.) or oral gavage
Result:T1/2s of 1.4, 5.0 and 13 h for mice, rats and dogs, respectively.

IC 50

TLR7: 11.1 nM (IC50, in HEK293 cells); TLR8: 24.1 nM (IC50, in HEK293 cells); TLR7: 68.3 nM (IC50, in peripheral blood mononuclear cells (PBMCs)); TLR8: 620 nM (IC50, in peripheral blood mononuclear cells (PBMCs)); TLR7: 2.2 nM (IC50, in whole blood (WB) cells); TLR8: 120 nM (IC50, in whole blood (WB) cells)

References

[1] Jaromir Vlach, et al. Discovery of M5049: A Novel Selective TLR7/8 Inhibitor for Treatment of Autoimmunity. J Pharmacol Exp Ther. 2020 Dec 16;JPET-AR-2020-000275. DOI:10.1124/jpet.120.000275

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- Preparation Products And Raw materials

Raw materials

Preparation Products

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- Suppliers

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View Lastest Price from 8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- pictures 2026-07-20 8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]-
2101938-42-3
1KG 98% 1000kg Shaanxi Dideu New Materials Co. Ltd

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- Spectrum

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]- inhibit,M5049,Inhibitor,Toll-like Receptor (TLR),M-5049,autoimmunity,M 5049,TLR7/8,selective,Enpatoran 5-((3R,5S)-3-Amino-5-(trifluoromethyl)piperidin-1-yl)quinoline-8-carbonitrile Enpatoran, 10 mM in DMSO Enpatoran/ M5049 5-[(3R,5S)-3-Amino-5-(trifluoromethyl)-1-piperidyl]quinoline-8-carbonitrile Enpatoran M5049 2101938-42-3