Cat. No.: HY-100851

LY-272015

LY-272015 is an orally active and selective 5-HT_2B receptor antagonist. LY-272015 blocks 5-HT₂ receptors and inhibits Fluoxetine (HY-B0102)-induced PDGFβ receptor transactivation. LY-272015 attenuates 5-HT-induced smooth muscle cell migration and proliferation, and inhibits downstream mTOR/p70S6K phosphorylation. LY-272015 reduces 5-HT-induced vasoconstriction. LY-272015 reverses the excitatory effect of BW-723C86 (HY-101369) on NTS neurons. LY-272015 lowers mean arterial blood pressure in severely hypertensive DOCA-salt rats. LY-272015 can be used in research related to diseases such as hypertension and cardiovascular calcification.

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

CAS No.: 159730-07-1
Formula: C₂₁H₂₄N₂O₂
Molecular Weight:336.43

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (286 KB)

LY-272015 Chemical Structure

CAS No.: 159730-07-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

5-HT_2B Receptor

PDGFRβ

mTOR

All 5-HT Receptor Isoforms :

All mTOR Isoforms :

All PDGFR Isoforms :

In Vitro

LY-272015 (LY) (0-5 μM; 5 min) inhibits Fluoxetine (HY-B0102)-induced PDGFβ receptor transactivation in SH-SY5Y cells^[1].
LY-272015 (100 nmol/L; 0-24 h) attenuates 5-HT-induced migration and proliferation of rat aortic SMCs^[2].
LY-272015 (10 nmol/L; 2 h) antagonizes 5-HT-induced activation of the mTOR/p70S6K pathway in rat aortic SMCs^[2].
LY 272015 (2.87 μg/mL; 5 min) had no significant effect on the amplitude or frequency of phrenic nerve discharge in isolated perfused brainstem preparations from Sprague-Dawley rats^[3].
LY-272015 right-shifted the BW-723C86 (HY-101369)-induced contraction curve in endothelium-denuded mesenteric arteries of DOCA-salt rats, confirming the involvement of vascular 5-HT_2B receptors in the increase^[4].

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

Western Blot Analysis^[1]

Cell Line:

SH-SY5Y
Concentration:

0, 0.01, 0.1, 0.5, 5 μM
Incubation Time:

5 min
Result:

Did not significantly abrogate fluoxetine-induced PDGFβ receptor phosphorylation at lower concentrations.
Inhibited fluoxetine-induced PDGFβ receptor phosphorylation at 5 μM.

Cell Migration Assay ^[2]

Cell Line:

Rat aortic smooth muscle cells (SMCs)
Concentration:

100 nmol/L
Incubation Time:

0, 24 h
Result:

Mitigated the 5-HT-induced migration of SMCs.\nLargely abrogated the enhancing effect of 5-HT on PDGF-BB-induced SMC migration.

Cell Proliferation Assay^[2]

Cell Line:

Rat aortic smooth muscle cells (SMCs)
Concentration:

100 nmol/L
Incubation Time:

24 h
Result:

Mitigated the 5-HT-induced proliferation of SMCs.

Western Blot Analysis^[2]

Cell Line:

Rat aortic smooth muscle cells (SMCs)
Concentration:

10 nmol/L
Incubation Time:

2 h (pre-treatment); 0, 2, 5, 15, 30, 60 min (5-HT stimulation)
Result:

Antagonized the 5-HT-induced phosphorylation of mTOR and p70S6K.

In Vivo

LY-272015 (0.3-3 mg/kg; intravenous injection; once weekly; for 4 weeks) significantly reduced mean arterial blood pressure in severely hypertensive DOCA-salt rats^[4].
LY-272015 (30-50 nA) reverses the excitatory effect of BW-723C86 on active Group 2 and Group 3 (active and inactive) NTS neurons, but does not reverse the inhibitory effect of BW-723C86 on inactive Group 2 cells^[5].
LY-272015 (3 mg/kg; intraperitoneal injection; 3 days per week; 8 weeks) did not inhibit the progression of aortic calcification or reduce atherosclerotic lipid/lesion area in diet-induced calcific atherosclerosis Apoe^−/− mice, and did not affect bone density^[6].

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

Animal Model:

Sprague-Dawley (Male, 300-350 g, DOCA-salt hypertension model)^[4]
Dosage:

0.3, 1.0, and 3.0 mg/kg
Administration:

i.v.; once per week; 4 weeks
Result:

Did not reduce blood pressure in sham-treated rats at any time or dose.
Did not cause blood pressure reduction in any group during weeks 1 and 2.
Reduced blood pressure by ~20 mmHg with 1.0 and 3.0 mg/kg in DOCA-S group at week 3.
Reduced blood pressure with 1.0 mg/kg and caused a significant fall in blood pressure (>40 mmHg) with 3.0 mg/kg after 30 min in week 4 DOCA-S rats.
Abolished the residual pressor response to α-methyl-5-HT after ketanserin in DOCA-S rats.
Did not alter the pressor response to phenylephrine in sham rats.
Abolished 5-HT-induced contraction in stomach fundus.

Animal Model:

Apoe^−/− (C57BL/6 background, male, 25 weeks old)^[6]
Dosage:

3 mg/kg
Administration:

i.p.; 3 days/week; 8 weeks
Result:

Did not inhibit aortic calcification progression, and produced no effects on lipid area, lesion area, or infiltration of CD68‑positive inflammatory cells.
Blocked the significant rise in systolic posterior left‑ventricular wall thickness, while leaving systolic‑diastolic left‑ventricular anterior wall thickness and diastolic posterior wall thickness unaffected; preserved week‑8 cardiac parameters including ejection fraction (67 %), fractional shortening (37 %), corrected LV mass (109 mg), LVAW systole (1.59 mm), LVAW diastole (1.09 mm), LVPW systole (1.34 mm), LVPW diastole (0.85 mm), and terminal body weight (40 g).
Reduced aortic HTR‑2A protein levels and exerted no influence on HTR‑2B protein abundance.
Displayed bone loss at study endpoint that showed no statistical differences relative to other experimental groups.

Animal Model:

Apoe^−/− (C57BL/6 background, female, 23 weeks old)^[6]
Dosage:

3 mg/kg
Administration:

i.p.; 3 days/week; 8 weeks
Result:

Did not inhibit the progression of aortic calcification and failed to reduce lipid content or atherosclerotic lesion area, and exerted no observable influence on the infiltration of CD68‑positive inflammatory cells.
Blocked the increases in systolic and diastolic anterior left‑ventricular wall thickness, while leaving systolic and diastolic posterior‑wall thickness unchanged; maintained stable cardiac functional indices including ejection fraction, fractional shortening, corrected LV mass and ventricular wall dimensional parameters at week 8.
Reduced aortic HTR‑2A protein expression levels but produced no change in HTR‑2B protein abundance.
Did not trigger bone loss in experimental animals at the end of the 8‑week experimental period.

Related Protocols :

Chemical Information

CAS No. 159730-07-1
Molecular Weight 336.43
Formula C₂₁H₂₄N₂O₂
SMILES

CC1=CC2=C(NC3=C2CCNC3CC4=CC=C(OC)C(OC)=C4)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kruk JS, et al. Fluoxetine-induced transactivation of the platelet-derived growth factor type β receptor reveals a novel heterologous desensitization process. Molecular and cellular neurosciences. 2015 Mar;65:45-51.

[2]. Liu Y. Inhibition of 5‐Hydroxytryptamine Receptor 2B Reduced Vascular Restenosis and Mitigated the β‐Arrestin2–Mammalian Target of Rapamycin/p70S6K Pathway. Journal of the American Heart Association. 2018 Jan 30;7(3):e006810.

[3]. Niebert M. Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network. PLoS One. 2011 Jul 18;6(7):e21395.

[4]. Watts SW, et al. 5-HT2B-receptor antagonist LY-272015 is antihypertensive in DOCA-salt-hypertensive rats. The American journal of physiology. 1999 Mar;276(3):H944-52. [Content Brief]

[5]. Sévoz-Couche C, et al. In vivo modulation of vagal-identified dorsal medullary neurones by activation of different 5-Hydroxytryptamine(2) receptors in rats. Br J Pharmacol. 2000 Dec;131(7):1445-53.

[6]. Hon A, et al. Specific serotonin receptor antagonist reduces murine calcific atherosclerosis. Atherosclerosis. 2026 Mar;414:120649.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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LY-272015

All 5-HT Receptor Isoforms

All mTOR Isoforms

All PDGFR Isoforms