CU-CPT-9b free base

CU-CPT9b is a specific TLR8 antagonist.

For research use only. Not for human or veterinary use.

Target Toll-like Receptor (TLR)

Research area Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

CU-CPT-9b structure

CAS No.: 2162962-69-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 450.00	BP-01977-500mg	In stock	Get quote
1 g	USD 680.00	BP-01977-1g	In stock	Get quote
5 g	Inquire	BP-01977-5g	In stock	Inquire

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Description

CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.

Biological activity

In Vitro CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7±0.2 nM. ITC experiments have confirmed the strong binding of CU-CPT9b with a Kd of 21 nM. It is shown that CU-CPT-9b binds to the inactive TLR8 dimer in a similar way to CU-CPT8m. CU-CPT9b utilizes hydrogen bonds with G351 and V520*, which are conserved among TLR8/antagonist structures. Additionally, CU-CPT9b forms water-mediated contacts with S516* and Q519*, which are not observed in TLR8/CU-CPT8m structure, suggesting that the enhanced potency of CU-CPT9b derives from the new interactions with these polar residues. The orientation of Y567* also changes to facilitate van der Waals interactions with CU-CPT9b as compared to TLR8/CU-CPT8m.

Identifiers

SMILES: CC1=CC(=CC=C1O)C1=CC=NC2=CC(O)=CC=C12
InChIKey: QXFYDRYRLOHSBD-UHFFFAOYSA-N

Specifications

MW (average): 251.2799
Formula: C₁₆H₁₃NO₂
CAS No.: 2162962-69-6
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Zhang S, et al. Small-molecule inhibition of TLR8 through stabilization of its resting state. Nat Chem Biol. 2018 Jan;14(1):58-64.

Same target

Search Toll-like Receptor (TLR)

Same research area

Search Inflammation/Immunology