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Dalazatide TFA

Cat. No. M31052
Dalazatide TFA Structure
Synonym:

ShK-186 TFA

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Quality Control & Documentation
Biological Activity

Dalazatide (ShK-186) TFA is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide TFA can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.

Chemical Information
Molecular Weight 4556.1
Formula C186H297F3N57PS7
Form Solid
Solubility (25°C) Water
Storage Store at ≤ -20°C, dry, sealed
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] Seow Theng Ong, et al. Front Pharmacol. Mechanisms Underlying C-type Inactivation in Kv Channels: Lessons From Structures of Human Kv1.3 and Fly Shaker-IR Channels

[2] Anu Tyagi, et al. Proc Natl Acad Sci U S A. Rearrangement of a unique Kv1.3 selectivity filter conformation upon binding of a drug

[3] Gabor Tajti, et al. Biochem Pharmacol. The voltage-gated potassium channel KV1.3 as a therapeutic target for venom-derived peptides

[4] Peter J Prentis, et al. Toxins (Basel). Sea Anemones: Quiet Achievers in the Field of Peptide Toxins

[5] Eric J Tarcha, et al. PLoS One. Safety and pharmacodynamics of dalazatide, a Kv1.3 channel inhibitor, in the treatment of plaque psoriasis: A randomized phase 1b trial

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Keywords: Dalazatide TFA, ShK-186 TFA supplier, Potassium Channel, inhibitors, activators


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