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CRX-527

Cat. No. M10331
CRX-527 Structure
Synonym:

CRX527

Size Price Availability
1mg USD 450  USD450 Custom Synthesis
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Quality Control & Documentation
Biological Activity

CRX-527 is a highly specific and potent TLR4 agonist, which displays significantly less toxicity when compared to LPS. CRX-527 activates Toll-like receptor 4 (TLR4). Subsequently, it initiates MyD88- and TRIF-dependent pro-inflammatory signaling cascades. Importantly, CRX-527 does not require the TLR4 co-receptor CD14 for activation of either signaling pathway. CRX-527, along with other AGPs, is less toxic than LPS and importantly retains its immunostimulatory properties.

Chemical Information
Molecular Weight 1488.04
Formula C81H151N2O19P
CAS Number 216014-14-1
Solubility (25°C) DMSO 1 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] Amandine Legat, et al. Eur J Immunol. CD14-independent responses induced by a synthetic lipid A mimetic

[2] Axel G Stover, et al. J Biol Chem. Structure-activity relationship of synthetic toll-like receptor 4 agonists

[3] Zi Yan Tan, et al. Open J Immunol. Synthetic TLR4 agonist as a potential immunotherapy for melioidosis

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