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Cl-amidine 

Cat. No. M30880
Cl-amidine  Structure
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Biological Activity

Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.

Chemical Information
Molecular Weight 310.78
Formula C14H19ClN4O2
CAS Number 913723-61-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Ming Zhai, et al. Nat Commun. Extracellular traps from activated vascular smooth muscle cells drive the progression of atherosclerosis

[2] Jianxin Du, et al. Hum Cell. Cl-amidine attenuates lipopolysaccharide-induced inflammation in human gingival fibroblasts via the JNK/MAPK, NF-κB, and Nrf2 signalling pathways

[3] Dina Ahmed, et al. Int J Mol Sci. Controlled Delivery of Pan-PAD-Inhibitor Cl-Amidine Using Poly(3-Hydroxybutyrate) Microspheres

[4] Chaoqun Wang, et al. Microb Pathog. Cl-amidine attenuates lipopolysaccharide-induced mouse mastitis by inhibiting NF-κB, MAPK, NLRP3 signaling pathway and neutrophils extracellular traps release

[5] Ali Z Siddiqui, et al. Surg Infect (Larchmt). Cl-Amidine Improves Survival and Attenuates Kidney Injury in a Rabbit Model of Endotoxic Shock

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Abmole Inhibitor Catalog




Keywords: Cl-amidine  supplier, PAD, inhibitors, activators

 
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