TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

Product information

CAS Number: 1642857-69-9

Molecular Weight: 336.35

Formula: C17H16N6O2

Chemical Name: 4-[(5-methyl-1,2-oxazol-3-yl)methoxy]-5-[(pyridin-2-yl)methyl]-5H-pyrrolo[3,2-d]pyrimidin-2-amine

Smiles: CC1=CC(COC2=NC(N)=NC3C=CN(CC4=CC=CC=N4)C=32)=NO1

InChiKey: FVKOYFLAKSGBBV-UHFFFAOYSA-N

InChi: InChI=1S/C17H16N6O2/c1-11-8-13(22-25-11)10-24-16-15-14(20-17(18)21-16)5-7-23(15)9-12-4-2-3-6-19-12/h2-8H,9-10H2,1H3,(H2,18,20,21)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 160 mg/mL (475.69 mM; Need ultrasonic and warming).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) of 0.4 μM in HEK293 cell. TLR7 agonist 2 is found to be selective for TLR7 over TLR8 with LEC of >100 μM for human TLR8. TLR7 agonist 2 demonstrates low inhibition across five CYP450 isozymes (IC50 >10 μM) and is also not a time dependent inhibitor of CYP450 3A4. TLR7 agonist 2 has limited inhibition of the hERG potassium ion channel 3H-dofetilide binding in vitro (IC50 >50 μM).

In Vivo:

TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both Cmax and AUC increase less than dose proportionally between 0.3 and 3 mg/kg and more than dose-proportionally between 3 and 10 mg/kg. TLR7 agonist 2 can induce an antiviral interferon stimulated gene (ISG) response without inducing an IFNα response at a low dose. TLR7 agonist 2 also induces a 2.7 log decrease in serum HBV viral load from 0.3 mg/kg, and a maximum 3.1 log decrease is observed for doses between 1 and 5 mg/kg.

Products are for research use only. Not for human use.