1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Adrenergic Receptor
  3. LY 344864

LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.

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LY 344864 Chemical Structure

LY 344864 Chemical Structure

CAS No. : 186544-26-3

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 77 In-stock
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10 mg USD 110 In-stock
50 mg USD 380 In-stock
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Description

LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent[1].

IC50 & Target[1]

human 5-HT1F Receptor

0.006 μM (Ki)

human 5-HT1A Receptor

0.530 μM (Ki)

human 5-HT1B Receptor

0.549 μM (Ki)

human 5-HT1D Receptor

0.575 μM (Ki)

human 5-HT1E Receptor

1.415 μM (Ki)

human 5-HT2B Receptor

1.695 μM (Ki)

Human 5-HT2A Receptor

3.499 μM (Ki)

Human 5-HT3A Receptor

3.935 mM (Ki)

Human 5-HT7 Receptor

4.851 μM (Ki)

rat α2-adrenergic receptor

3.69 μM (Ki)

rat α1-adrenergic receptor

5.06 μM (Ki)

In Vitro

LY 344864 binds to human 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT3A, 5-HT2B, 5-HT2C, 5-HT7, rat α1-adrenergic, rat α2-adrenergic receptors with Kis of 0.006, 0.530, 0.549, 0.575, 1.415, 3.935, 1.695, 3.499, 4.851, 5.06 and 3.69 μM, respectively[1].
LY 344864 is a inducer of mitochondrial biogenesis[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LY 344864 (0-10 ng/kg; p.o. or i.v.; once) inhibits neurogenic dural inflammation in rat migraine pain model[1].
LY 344864 (1 mg/kg; i.v.; once) can cross the blood brain barrier to some extent in rats[1].
LY 344864 (2 mg/kg; i.p.; daily for 14 days) attenuates dopaminergic neuron loss and improved behavioral endpoints in a Parkinson’s disease mouse model[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats, migraine pain model[1]
Dosage: 1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous)
Administration: Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation
Result: When given intravenously 10 minutes before stimulation, inhibited inflammation with an ID50 (median infective dose) of 0.6 ng/kg. When administered orally 75 minutes before trigeminal stimulation, an ID50 of 1.2 ng/kg was obtained.
Animal Model: Male C57BL/6 mice, Parkinson’s disease model[2]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection, daily for 14d beginning 7d post-lesion
Result: Attenuated TH-ir loss in the striatum and substantia nigra compared to vehicle-treated lesioned animals, also increased locomotor activity in 6-hydroxydopamine lesioned mice, while vehicle treatment had no effect.
Molecular Weight

351.42

Formula

C21H22FN3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC2=C(NC3=C2C[C@H](N(C)C)CC3)C=C1)C4=CC=C(F)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 100 mg/mL (284.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8456 mL 14.2280 mL 28.4560 mL
5 mM 0.5691 mL 2.8456 mL 5.6912 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.93%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8456 mL 14.2280 mL 28.4560 mL 71.1399 mL
5 mM 0.5691 mL 2.8456 mL 5.6912 mL 14.2280 mL
10 mM 0.2846 mL 1.4228 mL 2.8456 mL 7.1140 mL
15 mM 0.1897 mL 0.9485 mL 1.8971 mL 4.7427 mL
20 mM 0.1423 mL 0.7114 mL 1.4228 mL 3.5570 mL
25 mM 0.1138 mL 0.5691 mL 1.1382 mL 2.8456 mL
30 mM 0.0949 mL 0.4743 mL 0.9485 mL 2.3713 mL
40 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7785 mL
50 mM 0.0569 mL 0.2846 mL 0.5691 mL 1.4228 mL
60 mM 0.0474 mL 0.2371 mL 0.4743 mL 1.1857 mL
80 mM 0.0356 mL 0.1778 mL 0.3557 mL 0.8892 mL
100 mM 0.0285 mL 0.1423 mL 0.2846 mL 0.7114 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
LY 344864
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HY-13788
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