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GS-9876 (lanraplenib)

Cat. No. M20799
GS-9876 (lanraplenib) Structure
Synonym:

GS-SYK

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Biological Activity

Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

Chemical Information
Molecular Weight 443.5
Formula C23H25N9O
CAS Number 1800046-95-0
Solubility (25°C) DMSO 89 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Su'an Tang, et al. Expert Opin Investig Drugs. Investigational spleen tyrosine kinase (SYK) inhibitors for the treatment of autoimmune diseases

[2] Peter Blomgren, et al. ACS Med Chem Lett. Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases

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Keywords: GS-9876 (lanraplenib), GS-SYK supplier, Syk, inhibitors, activators

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