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Afimetoran

Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs) . Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus) [1][2].

Product Specifications

CAS Number

[2171019-55-7]

Product Name Alternative

BMS-986256

UNSPSC

12352005

Hazard Statement

H315, H319

Target

Apoptosis; NF-κB; Toll-like Receptor (TLR)

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/afimetoran.html

Purity

99.37

Solubility

DMSO : 100 mg/mL (ultrasonic; adjust pH to 2 with HCl) |Ethanol : 2 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(CN1CCC(CC1)C2=CC=C3NC(C4=CN5N=CN=C5C(C)=C4C)=C(C(C)C)C3=C2)N

Molecular Formula

C26H32N6O

Molecular Weight

444.57

Precautions

H315, H319

References & Citations

[1]Zhao Q, et al. POS1129 IN VITRO EVIDENCE DEMONSTRATES THAT AFIMETORAN (BMS-986256), AN EQUIPOTENT TLR7/8 DUAL ANTAGONIST, HAS STEROID-SPARING POTENTIAL IN THE CLINIC[J]. 2023.|[2]Dudhgaonkar S, et al. PO. 1.1 Afimetoran, a potent and selective inhibitor of human toll-like receptor 7 (TLR7) and tlr8, provides robust efficacy in a murine lupus model of advanced disease[J]. 2022.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Available Sizes

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