BMS-986256

Product Name: BMS-986256
CAS No.: 2171019-55-7
Chemical Name: BMS-986256
Synonyms: BMS-986256;Afimetoran（BMS-986256）;Afimetoran, 10 mM in DMSO;Toll-like Receptor (TLR),Afimetoran,BMS 986256,inhibit,BMS986256,Inhibitor;2-(4-(2-(7,8-Dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-isopropyl-1H-indol-5-yl)piperidin-1-yl)acetamide;1-Piperidineacetamide, 4-[2-(7,8-dimethyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-(1-methylethyl)-1H-indol-5-yl]-;2-(4-(2-(7,8-dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-(propan-2-yl)-1H-indol-5-yl)piperidin-1-yl)acetamide
CBNumber: CB98381869
Molecular Formula: C26H32N6O
Formula Weight: 444.57
MOL File: 2171019-55-7.mol

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BMS-986256 Property

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)
pka: 15.19±0.30(Predicted)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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BMS-986256 Chemical Properties,Usage,Production

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.

BMS-986256 Preparation Products And Raw materials

Raw materials

Preparation Products

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BMS-986256 Suppliers

China 29 United States 4 Global 33

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2171019-55-7, BMS-986256Related Search:

1-Piperidineacetamide, 4-[2-(7,8-dimethyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-(1-methylethyl)-1H-indol-5-yl]-

BMS-986256

Toll-like Receptor (TLR),Afimetoran,BMS 986256,inhibit,BMS986256,Inhibitor

2-(4-(2-(7,8-Dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-isopropyl-1H-indol-5-yl)piperidin-1-yl)acetamide

2-(4-(2-(7,8-dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-(propan-2-yl)-1H-indol-5-yl)piperidin-1-yl)acetamide

Afimetoran（BMS-986256）

Afimetoran, 10 mM in DMSO

2171019-55-7