| Identification | Back Directory | [Name]
BMS-986256 | [CAS]
2171019-55-7 | [Synonyms]
BMS-986256
1-Piperidineacetamide, 4-[2-(7,8-dimethyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-(1-methylethyl)-1H-indol-5-yl]- | [Molecular Formula]
C26H32N6O | [MOL File]
2171019-55-7.mol | [Molecular Weight]
444.57 |
| Chemical Properties | Back Directory | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (224.94 mM; ultrasonic and adjust pH to 2 with HCl) | [form ]
Solid | [pka]
15.19±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Afimetoran (0.25 mg/kg; once daily; p.o.) shows strong therapeutic effects in late lupus mouse models by inhibiting the activation of TLR7/8[2]. | Animal Model: | NZB/W mice with advanced lupus (proteinuria > 100 mg/dL)[2]. | | Dosage: | 0.25 mg/kg | | Administration: | Oral gavage (p.o.); once daily | | Result: | Reversed kidney tissue damage, proteinuria, the number of IgG positive glomeruli, and the deposition of IgG in glomeruli, and reduced cytokine secreting cells and cytokines, resulting in a nearly complete (92%) survival rate. |
| [IC 50]
TLRs | [References]
[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. |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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