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Chemical Structure| 1800046-95-0 Chemical Structure| 1800046-95-0

Structure of Lanraplenib
CAS No.: 1800046-95-0

Chemical Structure| 1800046-95-0

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Lanraplenib (GS-9876) is a highly selective oral SYK inhibitor with an IC50 of 9.5 nM, used for the study of inflammatory diseases.

Synonyms: GS-9876; GS-SYK

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Product Details of Lanraplenib

CAS No. :1800046-95-0
Formula : C23H25N9O
M.W : 443.50
SMILES Code : NC1=CN=CC(C2=CN3C(C(NC4=CC=C(N5CCN(C6COC6)CC5)C=C4)=N2)=NC=C3)=N1
Synonyms :
GS-9876; GS-SYK

Safety of Lanraplenib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Lanraplenib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human B cells 245 nM 7 days Lanraplenib dose-dependently inhibited B cell maturation with an EC50 value of 245 nM. BMC Rheumatol. 2021 Mar 30;5(1):15
Human B cells 298 nM (HD), 340 nM (SLE) 16 hours Lanraplenib dose-dependently inhibited CD69 expression with EC50 values of 298 nM (healthy donors) and 340 nM (SLE patients). BMC Rheumatol. 2021 Mar 30;5(1):15
Human B cells 130 nM 48 hours Lanraplenib dose-dependently reduced B cell survival with an EC50 value of 130 nM. BMC Rheumatol. 2021 Mar 30;5(1):15
J774 macrophages 2 μM 30 min Inhibition of Syk kinase activity, reducing intracellular Ca2+ flashing Mol Biol Cell. 2024 Jan 1;35(1):ar5
Human B cells 216 nM 7 days Lanraplenib dose-dependently inhibited IgM secretion with an EC50 value of 216 nM. BMC Rheumatol. 2021 Mar 30;5(1):15

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NZB/W mice Systemic lupus erythematosus and lupus nephritis model Oral 0.25% in chow Continuous administration until study end Lanraplenib treatment significantly improved overall survival, prevented the development of proteinuria, and reduced blood urea nitrogen concentrations in NZB/W mice. BMC Rheumatol. 2021 Mar 30;5(1):15

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.23mL

11.27mL

2.25mL

1.13mL

22.55mL

4.51mL

2.25mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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