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Lasmiditan

Cat. No. M10160
Lasmiditan Structure
Synonym:

COL-144; LY573144

Size Price Availability Quantity
2mg USD 55  USD55 In stock
5mg USD 80  USD80 In stock
10mg USD 120  USD120 In stock
50mg USD 350  USD350 In stock
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Quality Control
Biological Activity

Lasmiditan (COL-144; LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist, showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor in vitro binding studies. Lasmiditan showed higher selectivity for the 5-HT(1F) receptor relative to other 5-HT(1) receptor subtypes than the first generation 5-HT(1F) receptor agonist LY334370. In two rodent models of migraine, oral administration of lasmiditan potently inhibited markers associated with electrical stimulation of the trigeminal ganglion (dural plasma protein extravasation, and induction of the immediate early gene c-Fos in the trigeminal nucleus caudalis).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 377.14
Formula C19H18F3N3O2
CAS Number 439239-90-4
Purity 99.82%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

[1] Jasper Mecklenburg, et al. Ther Adv Neurol Disord. The potential of lasmiditan in migraine

[2] David L Nelson, et al. Cephalalgia. Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan

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Keywords: Lasmiditan, COL-144; LY573144 supplier, 5-HT Receptor, inhibitors

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