1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Lasmiditan hydrochloride

Lasmiditan hydrochloride (Synonyms: LY 573144 hydrochloride; COL-144 hydrochloride)

Cat. No.: HY-14861A Purity: 99.91%
Handling Instructions

Lasmiditan hydrochloride is a high-affinity, highly selective 5-HT1F receptor agonist (Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.

For research use only. We do not sell to patients.

Lasmiditan hydrochloride Chemical Structure

Lasmiditan hydrochloride Chemical Structure

CAS No. : 613677-28-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Lasmiditan hydrochloride is a high-affinity, highly selective 5-HT1F receptor agonist (Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively[1].

IC50 & Target

Ki: 2.1 nM (5-HT1F), >1000 nM (5-HT1B/5-HT1D)[1]

In Vitro

In vitro binding studies Lasmiditan showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor, compared with K(i) values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan show 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. Unlike the 5-HT(1B/1D) receptor agonist sumatriptan, lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 μM[1].

In Vivo

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)[2].

Clinical Trial
Molecular Weight

413.82

Formula

C₁₉H₁₉ClF₃N₃O₂

CAS No.

613677-28-4

SMILES

O=C(NC1=NC(C(C2CCN(C)CC2)=O)=CC=C1)C3=C(F)C=C(F)C=C3F.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (67.66 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4165 mL 12.0825 mL 24.1651 mL
5 mM 0.4833 mL 2.4165 mL 4.8330 mL
10 mM 0.2417 mL 1.2083 mL 2.4165 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LasmiditanLY 573144COL-144LY573144LY-573144COL144COL 1445-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Product name:
Lasmiditan hydrochloride
Cat. No.:
HY-14861A
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