| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| Targets |
5-HT1F Receptor ( Ki = 1.6 nM )
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|---|---|
| ln Vitro |
LY334370 does not exhibit vasoconstrictor effects on human cerebral arteries in vitro, unless it is administered at a dose of 10-5 M, at which point it causes an 8.5±5.7% contraction, which is not statistically significant[1].
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| ln Vivo |
Intravenous LY334370 administration at 3 mg/kg (n = 3) or 10 mg/kg (n = 6) causes an increase in dural blood vessel diameter of 135±6% and 106±11%, respectively, after electrical stimulation; these values do not differ significantly from the corresponding control values. Since dural blood vessel diameter is actually 43±4 arbitrary units before drug injection and 43±4 arbitrary units 15 minutes after injection of LY334370 (10 mg/kg), LY334370 has no effect on dural blood vessel diameter per se[1].
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| Cell Assay |
In this study, human cerebral arteries are used. Segments are prepared as previously described, but briefly they are placed in a buffer solution containing (mM) NaCl 119, NaHCo3 15, KCl 4.6, CaCl2 1.5, NaH2PO4 1.2, MgCl2 1.2, and glucose 5.5. Sections of the vessel, measuring 0.5 mm in diameter and 1 to 2 mm in length, are placed in a tissue bath that is heated to 37°C and contains a buffer solution that has been agitated with 5% CO2 and 95% O2. Four mN of tension is applied to the vessel segments, and they are left to stabilize there for one to one and a half hours. Exposure to 60 mM KCl is used to test the reactivity of vessels. Only if the response is similar to the segment used for LY334370 testing is this repeated twice for each segment. As a percentage of the maximum KC1 response, responses to LY334370 are computed[1].
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| Animal Protocol |
There are 300–400 g male Sprague-Dawley rats used. Intravital microscopy and a video dimension analyzer are used to measure the diameter of a branch of the middle meningeal artery in the intact skull of rats housed in a stereotaxic frame after their skulls have been thinned and exposed through drilling. A bipolar stimulating electrode, positioned on the cranial window surface about 200 μM away from the vessel of interest, is used to induce neurogenic vasodilation. After LY334370 (3 or 10 mg/kg, iv.) is administered five minutes after an electrical stimulation response that produces a control vasodilation is produced, and after another fifteen minutes, the electrical stimulation is repeated. For each response, the mean maximum percentage increase in dural vessel diameter relative to the pre-stimulus baseline is calculated. Analysis of variance is then used to compare the vasodilation responses evoked in the presence or absence of LY334370, and paired t-tests are employed to make these comparisons[1].
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| References |
| Molecular Formula |
C21H22FN3O
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|---|---|
| Molecular Weight |
351.41728
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| Exact Mass |
351.17
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| CAS # |
182563-08-2
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| Related CAS # |
199673-74-0(LY334370 hydrochloride)
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| Appearance |
White to off-white solid powder
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| SMILES |
CN1CCC(CC1)C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F
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| InChi Key |
MDMJLMDBRQXOOI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22FN3O/c1-25-10-8-14(9-11-25)19-13-23-20-7-6-17(12-18(19)20)24-21(26)15-2-4-16(22)5-3-15/h2-7,12-14,23H,8-11H2,1H3,(H,24,26)
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| Chemical Name |
4-fluoro-N-[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]benzamide
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| Synonyms |
LY334370
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 55.5 mg/mL (~157.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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