Biological Activity

Anakinra (Raleukin) is an antagonist of recombinant, nonglycosylated human IL-1R. Anakinra is the first biological agent to block the pro-inflammatory effects. In vivo, combined Etanercept (5 mg/kg, ip) and Anakinra (100 mg/kg, ip. daily for 7 days) substantially improves marginal mass human islet engraftment in immunodeficient mice. Anakinra enhances tumor growth inhibition in mice receiving peptide vaccination and β-(1-3),(1-6)-D-glucan.

Product Citations

• 

  Cell Biosci. 2022 Jun 17;12(1):90.

  IL-1R/C3aR signaling regulates synaptic pruning in the prefrontal cortex of depression
  Anakinra purchased from AbMole

Chemical Information

Molecular Weight	509.56
Formula	C20H23N5O7S2
CAS Number	143090-92-0
Storage	2-8°C, do not freeze

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] B Naziruddin, et al. Am J Transplant. Improved outcomes of islet autotransplant after total pancreatectomy by combined blockade of IL-1β and TNFα

[2] M McCall, et al. Am J Transplant. Anakinra potentiates the protective effects of etanercept in transplantation of marginal mass human islets in immunodeficient mice

[3] Ulf Harnack, et al. Anticancer Res. IL-1 receptor antagonist anakinra enhances tumour growth inhibition in mice receiving peptide vaccination and beta-(1-3),(1-6)-D-glucan