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E6130

Cat. No. M14694
E6130 Structure
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Biological Activity

E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.

Chemical Information
Molecular Weight 556.06
CAS Number 1427058-33-0
Solubility (25°C) DMSO ≥ 150 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] Konstantin Hofmann, et al. Pregnancy management for a woman with extensive vulvar and pelvic malformations caused by Klippel-Trénaunay syndrome

[2] Eimear Mylod, et al. The Omentum in Obesity-Associated Cancer: A Hindrance to Effective Natural Killer Cell Migration towards Tumour Which Can Be Overcome by CX3CR1 Antagonism

[3] Eyad Mansour, et al. Arterial Thrombus in a Protein C Deficient Patient

[4] Hisashi Wakita, et al. E6130, a Novel CX3C Chemokine Receptor 1 (CX3CR1) Modulator, Attenuates Mucosal Inflammation and Reduces CX3CR1 + Leukocyte Trafficking in Mice with Colitis

[5] Bjrn Gerdle, et al. Signs of ongoing inflammation in female patients with chronic widespread pain: A multivariate, explorative, cross-sectional study of blood samples

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