RN486
Product Description
.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}
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]
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.
Protocol(Only for Reference)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.
Chemical Information
Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on RN486. We are ready to answer your questions on packaging, logistics, certification or any other aspects about RN486、RN486. If these products fail to match your need, please contact us and we would like to provide relevant information.
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 |
Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on RN486. We are ready to answer your questions on packaging, logistics, certification or any other aspects about RN486、RN486. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Angiogenesis > BTK Inhibitor
Other Products
Hot Products
Astragaloside AChlortetracycline HCl 64-72-2Paclitaxel 33069-62-4Dexamethasone Acetate 1177-87-3Dinaciclib (SCH727965) 779353-01-4CHIR-124 405168-58-3Ro3280 1062243-51-9TAME 901-47-3CCG-1423 285986-88-110058-F4 403811-55-2Dabigatran (BIBR 953) 211914-51-1H 89 2HCl 130964-39-5T0901317 293754-55-9Aprepitant 170729-80-3Turofexorate Isopropyl (XL335) 629664-81-9BMS-378806 357263-13-9