RN486

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Molecular Weight:

RN486 is a potent and selectivityBTK inhibitor, with IC50 of 4 nM.


Biological Activity


RN486 not only potently and selectively inhibits the Btk enzyme, but
also displays functional activities in human cell-based assays in
multiple cell types, blocking Fcε receptor cross-linking-induced
degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor
engagement-mediated tumor necrosis factor α production in monocytes
(IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an
activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM).
RN486 is able to block the signaling of BCR as demonstrated by a marked
inhibition of phosphorylation of both Btk and PLCγ2 in B cells. RN486
displays a selective B cell inhibitory profile in BioMAP Systems.


RN486 displays similar functional activities in rodent models,
effectively preventing type I and type III hypersensitivity responses.
More importantly, RN486 produces robust anti-inflammatory and
bone-protective effects in mouse CIA and rat adjuvant-induced arthritis
(AIA) models. In the AIA model, RN486 inhibits both joint and systemic
inflammation either alone or in combination with methotrexate, reducing
both paw Swelling and inflammatory markers in the blood.


Protocol(Only for Reference)


Kinase Assay:


[1]

Enzymatic Activity and Binding AssaysBtk Enzymatic Activity Assay.

A fluorescence-based kinase assay is used to measure Btk kinase activity and its inhibition by RN486. In the assay, test compound is incubated with a human recombinant Btk (10 nM), ATP (100 μM), and a fluorescent-labeled peptide substrate (15 μM) at 30°C for 15 min. The reaction is then stopped by the addition of a termination buffer, and reaction product is quantified by using a Desktop Profiler 4 sipper.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Protocol(Only for Reference)


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

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Product Categories : Angiogenesis > BTK Inhibitor