TLR8 agonist 2 is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 shows less active against human TLR7 (EC50 of 33.33 μM).

Product information

CAS Number: 2412937-64-3

Molecular Weight: 326.40

Formula: C16H22N8

Chemical Name: N4-[(2R)-2-methyl-1-(4H-1, 2, 4-triazol-3-yl)hexan-2-yl]pyrido[3, 4-d]pyrimidine-2, 4-diamine

Smiles: CCCC[C@](C)(CC1NC=NN=1)NC1=NC(N)=NC2=CN=CC=C21

InChiKey: MFXIZGDOEUUJFM-MRXNPFEDSA-N

InChi: InChI=1S/C16H22N8/c1-3-4-6-16(2,8-13-19-10-20-24-13)23-14-11-5-7-18-9-12(11)21-15(17)22-14/h5,7,9-10H,3-4,6,8H2,1-2H3,(H,19,20,24)(H3,17,21,22,23)/t16-/m1/s1

Technical Data

Appearance: Solid Power

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

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:

TLR8 agonist 2 (Example 1) increases the levels of TNF-α, IL-12p40, IFN-γ, and IFN-α with EC50 values 105 nM, 26 nM, 29 nM, and 2800 nM, respectively, in human peripheral blood mononuclear cells (hPBMC).

In Vivo:

The pharmacokinetic related parameters of TLR8 agonist 2 (Example 1) in mice administered with the intravenous administration of 1 mg/kg and the oral administration of 5 mg/kg are detected. The T1/2 of TLR8 agonist 2 are 0.25 h (1 mg/kg i.v.) and 0.5 h (5 mg/kg p.o.), the AUClast are 450 ng/mL*hr (i.v.) and 624 ng/mL*hr (p.o.). And for oral administration, the bioavailability (%F) is 27.7%

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