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sPLA2 inhibitor

Cat. No. M8168
sPLA2 inhibitor Structure
Size Price Availability
5mg USD 780  USD780 1-2 Weeks
10mg USD 1425  USD1425 1-2 Weeks
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Quality Control & Documentation
Biological Activity

Secretory phospholipase A2 inhibitor blocks the activation of NF-κB, Akt, p38 MAPK and ERK pathways. It reduces proliferation and induces apoptosis of lung cancer cells and is a potent anti-inflammatory agent. sPLA2 inhibitor prevents deposition of collagen and has anti-fibrotic effects in hypertensive rats.

Chemical Information
Molecular Weight 487.63
Formula C31H37NO4
CAS Number 393569-31-8
Solubility (25°C) DMSO: 20 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] Yongjun Guo, et al. sPLA2-IIA Augments Oxidized LDL-Induced MCP-1 Expression in Vitro Through Activation of Akt

[2] Shahar Lavi, et al. Inhibition of sPLA2 and endothelial function: a substudy of the SPIDER-PCI trial

[3] Yi Wei, et al. sPLA2-IIa amplifies ocular surface inflammation in the experimental dry eye (DE) BALB/c mouse model

[4] Paul A J Krijnen, et al. Inhibition of sPLA2-IIA, C-reactive protein or complement: new therapy for patients with acute myocardial infarction?

[5] Y Yokota, et al. Suppression of murine endotoxic shock by sPLA2 inhibitor, indoxam, through group IIA sPLA2-independent mechanisms

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