Art. -Nr.: HY-139567

Afimetoran

(Synonyms: BMS-986256)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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).

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Reinheit: 99.37%
CAS. Nr.: 2171019-55-7
Formel: C₂₆H₃₂N₆O
Molecular Weight:444.57

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Afimetoran Chemical Structure

CAS. Nr.: 2171019-55-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

TLRs

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2171019-55-7
Appearance Solid
Molecular Weight 444.57
Formel C₂₆H₃₂N₆O
Color White to off-white
SMILES

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

BMS-986256
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Mol Immunol

Inhibition of RNase L enhances the expression efficiency of mRNA-LNPs. [Abstract]

2026 Feb:190:101-109. PMID: 41564652

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (224.94 mM; ultrasonic and adjust pH to 2 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 2 mg/mL (4.50 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2494 mL

11.2468 mL

22.4936 mL

5 mM

0.4499 mL

2.2494 mL

4.4987 mL

10 mM

0.2249 mL

1.1247 mL

2.2494 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.2494 mL	11.2468 mL	22.4936 mL	56.2341 mL
DMSO	5 mM	0.4499 mL	2.2494 mL	4.4987 mL	11.2468 mL
	10 mM	0.2249 mL	1.1247 mL	2.2494 mL	5.6234 mL
	15 mM	0.1500 mL	0.7498 mL	1.4996 mL	3.7489 mL
	20 mM	0.1125 mL	0.5623 mL	1.1247 mL	2.8117 mL
	25 mM	0.0900 mL	0.4499 mL	0.8997 mL	2.2494 mL
	30 mM	0.0750 mL	0.3749 mL	0.7498 mL	1.8745 mL
	40 mM	0.0562 mL	0.2812 mL	0.5623 mL	1.4059 mL
	50 mM	0.0450 mL	0.2249 mL	0.4499 mL	1.1247 mL
	60 mM	0.0375 mL	0.1874 mL	0.3749 mL	0.9372 mL
	80 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7029 mL
	100 mM	0.0225 mL	0.1125 mL	0.2249 mL	0.5623 mL

Keywords

Afimetoran

1 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Afimetoran

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Afimetoran Related Classifications

HY-139567 Related Classifications