Art. -Nr.: HY-163565

BIIB129

Name: BIIB129
Brand: MedChemExpress
SKU: HY-163565
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BIIB129 is a covalent, selective, orally active, and brain-penetrant BTK inhibitor (K_d = 0.63 nM). BIIB129 binds to Cys481 and forms a hydrogen bond with Asn484, blocking BCR and FcγR signaling. BIIB129 inhibits B cell activation and proliferation, FcγR-induced microglial proliferation, FcγR-mediated ROS production in neutrophils, FcγR-induced TNF secretion in monocytes, and B cell-mediated antigen presentation to T cells. BIIB129 can be used for research on multiple sclerosis.

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Reinheit : 99.54%
CAS. Nr.: 2770960-52-4
Formel: C₁₉H₂₂N₆O₂
Molecular Weight:366.42

Speicherung:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

BIIB129 Chemical Structure

CAS. Nr.: 2770960-52-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
Microglia	EC₅₀	1.5 mg/kg Compound: 25; BI1B129	Inhibition of po dosed FcR binding anti-MOG antibodies treated mouse microglial proliferation administered twice daily Inhibition of po dosed FcR binding anti-MOG antibodies treated mouse microglial proliferation administered twice daily	[PMID: 38712838]
Monocyte	IC₅₀	3 nM Compound: 25; BI1B129	Inhibition of FcgammaR-mediated TNF secretion in monocytes (unknown origin) Inhibition of FcgammaR-mediated TNF secretion in monocytes (unknown origin)	[PMID: 38712838]
Neutrophil	IC₅₀	3.2 nM Compound: 25; BI1B129	Inhibition of FcgammaR-mediated ROS production in neutrophils (unknown origin) Inhibition of FcgammaR-mediated ROS production in neutrophils (unknown origin)	[PMID: 38712838]
PBMC	IC₅₀	13 nM Compound: 25; BI1B129	Inhibition of anti-IgD induced B-cell activation in human PBMCs Inhibition of anti-IgD induced B-cell activation in human PBMCs	[PMID: 38712838]
T-cell	IC₅₀	1.9 nM Compound: 25; BI1B129	Inhibition of OVA332 to 339 specific T-cells (unknown origin) proliferation assessed as reduction in B-cell mediated antigen presentation to T cells Inhibition of OVA332 to 339 specific T-cells (unknown origin) proliferation assessed as reduction in B-cell mediated antigen presentation to T cells	[PMID: 38712838]
TMD8	IC₅₀	0.82 nM Compound: 25; BI1B129	Inhibition of human TMD8 cells proliferation incubated for 35 to 72 hrs by CellTiter-Glo luminescent cell viability assay Inhibition of human TMD8 cells proliferation incubated for 35 to 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 38712838]
TMD8	IC₅₀	7.1 nM Compound: 25; BI1B129	Antiproliferative activity against human TMD8 cells by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human TMD8 cells by CellTiter-Glo luminescent cell viability assay	[PMID: 38712838]

In Vitro

BIIB129 potently inhibits B cell activation in human whole blood^[1].
BIIB129 potently inhibits TMD8 B cell proliferation^[1].
BIIB129 demonstrates moderate intrinsic clearance in rat and human liver microsomes^[1].
BIIB129 is highly selective for BTK over other kinases with a reactive cysteine at the 481 position^[1].
BIIB129 potently inhibits BCR signaling in Ramos B cells^[1].
BIIB129 inhibits NF-κB signaling in TMD8 cells^[1].
BIIB129 modulates CD19 and CD36 expression in TMD8 cells^[1].
BIIB129 inhibits FcγR signaling in monocytes^[1].
BIIB129 (25) inhibits basophil degranulation in human whole blood^[1].
BIIB129 potently blocks B cell-mediated antigen presentation to T cells^[1].

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

Parmacokinetics

Species	Dose	Route	V_dss	T_1/2	CL	F
Rat^[1]	1.5 mg/kg	i.v.	4.3 L/kg	3.59 h	87 mL/min/kg	25 %
Cynomolgus Monkey^[1]	5 mg/kg	i.v.	1.19 L/kg	0.29 h	53.5 mL/min/kg	/

In Vivo

BIIB129 (compound 25) (2.5-25 mg/kg; p.o.; twice daily; 2.5 days) shows efficacy in blocking BCR-mediated activation of compartmentalized B cells in the CNS in mice, with maximum inhibition observed at 25 mg/kg^[1].
BIIB129 (0.1-31.7 mg/kg; p.o.; twice daily) exhibits dose-dependent efficacy in inhibiting FcγR-induced microglial proliferation in mice, with an EC₅₀ of 1.5 mg/kg^[1].

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

Animal Model:

NOD.SCID mice (immunodeficient) injected with TMD8 cells^[1]
Dosage:

2.5 mg/kg, 10 mg/kg, 25 mg/kg
Administration:

p.o.; BID; 2.5 days
Result:

Induced a dose-response with maximal inhibition at 25 mg/kg.

Related Protocols :

Chemical Information

CAS. Nr. 2770960-52-4
Appearance Solid
Molecular Weight 366.42
Formel C₁₉H₂₂N₆O₂
Color White to off-white
SMILES

CN(N=C1)C=C1C2=CN3C(C(O[C@]4(C[C@H](C4)N(C)C(C=C)=O)C)=N2)=CC=N3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (136.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.7291 mL

13.6455 mL

27.2911 mL

5 mM

0.5458 mL

2.7291 mL

5.4582 mL

10 mM

0.2729 mL

1.3646 mL

2.7291 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 (stored under nitrogen). 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 (6.82 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.82 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 (293 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Himmelbauer MK, et al. Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis. Journal of medicinal chemistry. 2024 May 23;67(10):8122-8140. [Content Brief]

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7291 mL	13.6455 mL	27.2911 mL	68.2277 mL
	5 mM	0.5458 mL	2.7291 mL	5.4582 mL	13.6455 mL
	10 mM	0.2729 mL	1.3646 mL	2.7291 mL	6.8228 mL
	15 mM	0.1819 mL	0.9097 mL	1.8194 mL	4.5485 mL
	20 mM	0.1365 mL	0.6823 mL	1.3646 mL	3.4114 mL
	25 mM	0.1092 mL	0.5458 mL	1.0916 mL	2.7291 mL
	30 mM	0.0910 mL	0.4549 mL	0.9097 mL	2.2743 mL
	40 mM	0.0682 mL	0.3411 mL	0.6823 mL	1.7057 mL
	50 mM	0.0546 mL	0.2729 mL	0.5458 mL	1.3646 mL
	60 mM	0.0455 mL	0.2274 mL	0.4549 mL	1.1371 mL
	80 mM	0.0341 mL	0.1706 mL	0.3411 mL	0.8528 mL
	100 mM	0.0273 mL	0.1365 mL	0.2729 mL	0.6823 mL

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BIIB129