Cat. No.: HY-14604

Xaliproden hydrochloride

(Synonyms: SR57746A; SR57746 hydrochloride)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [³⁵S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.

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

Purity: 98.40%
CAS No.: 90494-79-4
Formula: C₂₄H₂₃ClF₃N
Molecular Weight:417.89

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Xaliproden hydrochloride Chemical Structure

CAS No.: 90494-79-4

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

5-HT_1A Receptor

D₂ Receptor

All 5-HT Receptor Isoforms :

All Dopamine Receptor Isoforms :

All Trk Receptor Isoforms :

All PKC Isoforms :

All ERK Isoforms :

All Akt Isoforms :

All JNK Isoforms :

In Vitro

Xaliproden hydrochloride (1-10 μM; 5-30 min) does not activate the TrkA receptor in rat pheochromocytoma PC12 cells^[1].
Xaliproden hydrochloride (1 μM; 5 min-48 h) induces time-dependent tyrosine phosphorylation of the p66^shc and p52^shc isoforms in rat pheochromocytoma PC12 cells, with the phosphorylation of p66^shc peaking at 5 min and that of p52^shc peaking at 48 h^[1].
Xaliproden hydrochloride (0.1-5 μM; 5-30 min) induces dose-dependent transient activation of ERK1/ERK2 MAP kinases in PC12 rat pheochromocytoma cells, with a 3-fold activation peak of ERK2 at 1 μM for 5 min, and the maximum activation level achieved at 5 μM for 5 min^[1].
Activation of ERK1/ERK2 MAP kinases and phosphorylation of PKC isoforms induced by xaliproden hydrochloride (1 μM; 5-30 min) in PC12 rat pheochromocytoma cells depend on PKC activity, whereas 5-HT_1A receptor antagonism or G_i/o protein inactivation inhibits PKC activation^[1].
Xaliproden hydrochloride (1-10 μM; 24 h) protects human renal proximal tubular epithelial cells from high glucose-induced injury by inhibiting the JNK/p65/c-Jun signaling pathway and alleviating inflammation, apoptosis and fibrosis^[2].
Xaliproden hydrochloride (10 μM) activates G proteins via native 5-HT_1areceptors in the rat hippocampus, lateral septum, frontal cortex and entorhinal cortex, and this effect is completely blocked by the 5-HT_1areceptor antagonist WAY100635 (HY-10349)^[4].

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

Western Blot Analysis^[1]

Cell Line:

PC12 rat pheochromocytoma cells
Concentration:

1 μM (Xaliproden); 1 μM, 5 μM (chelerythrine chloride, pre-incubation); 10 μM (pindobind, pre-incubation); 50 ng/mL (pertussis toxin, pre-incubation)
Incubation Time:

5 min (Xaliproden; following 1 h pre-incubation with chelerythrine chloride); 30 min (Xaliproden; following 1 h pre-incubation with pindobind or 2 h pre-incubation with pertussis toxin)
Result:

Pre-incubation with 1 μM or 5 μM chelerythrine chloride blocked Xaliproden-induced ERK1/ERK2 activation.
Pre-incubation with GF109203X repressed Xaliproden-induced ERK1/ERK2 activation.
Induced phosphorylation of PKC isoforms α, βI, βII, γ, δ at 30 min, which was inhibited by pre-incubation with pindobind or pertussis toxin.

Cell Viability Assay^[2]

Cell Line:

human renal proximal tubular epithelial cells (high glucose-stimulated)
Concentration:

1 μM, 10 μM
Incubation Time:

24 h (co-incubation with high glucose)
Result:

Did not affect cell viability of high glucose-stimulated cells.
Significantly reduced phosphorylation of JNK, p65, and c-Jun.
Decreased protein expression of inflammatory cytokines IL-1β, IL-6, and TNF-α.
Reduced the number of TUNEL-positive apoptotic cells.
Lowered protein levels of cleaved caspase-3 and cleaved PARP.
Decreased expression of fibrotic proteins TGF-β, phospho-Smad2/3, and collagen 1.
Produced comparable reductions in p-JNK, p-p65, inflammatory proteins, TUNEL-positive cells, apoptotic proteins, p-c-Jun, and fibrotic proteins when co-treated with SP600125 as when used alone.
Produced comparable reductions in p-c-Jun and fibrotic proteins when co-treated with SR11302 as when used alone.
Showed no dose-dependent effect between 1 μM and 10 μM concentrations.

In Vivo

Xaliproden extends the average survival time and improves motor function in pmn mice with hereditary axonopathy, and rescues motor neurons from death in mice with transected sciatic nerves^[1].
Xaliproden (0.3-1.5 mg/kg/day; oral administration; once daily; for 4 consecutive weeks) hydrochloride exerts renoprotective effects on db/db mice with diabetic nephropathy by significantly improving renal function, reducing proteinuria, alleviating renal tubular injury and fibrosis, as well as blocking inflammatory, apoptotic and fibrotic pathways via inhibition of the JNK/p65/c-Jun signaling axis^[2].
Xaliproden (0.3-3 mg/kg; p.o.; single administration) hydrochloride significantly, persistently and dose-dependently inhibits Paclitaxel (HY-B0015)-induced mechanical allodynia^[3].
Xaliproden (0.3-3 mg/kg; p.o.; single administration) hydrochloride exerts only a mild, transient 19% inhibition of vincristine (HY-N0488A)-induced mechanical allodynia at the single dose of 3 mg/kg, shows no effect at low doses, and does not alter the tibial nerve firing response in vincristine-treated mice^[3].
Xaliproden (0.63-40 mg/kg; p.o.; single administration) hydrochloride produces a dose-dependent inhibitory effect on in vivo 5-HT_1A receptor binding in the frontal cortex and hippocampus of mice, with ID₅₀ values of 3.5 mg/kg and 3.3 mg/kg (p.o.), respectively^[4].
Xaliproden (0.63-10 mg/kg; intraperitoneal injection; single administration) hydrochloride dose-dependently increases dopamine levels in the prefrontal cortex of rats (ED₅₀=0.7 mg/kg, i.p.) and decreases 5-HT levels in the rat hippocampus (ED₅₀=1.2 mg/kg, i.p.) via activation of the 5-HT_1A receptor^[4].
Xaliproden (0.63-10 mg/kg; intraperitoneal injection; single administration) hydrochloride exerts a dose-dependent, 5-HT_1A receptor-mediated antinociceptive effect in the rat formalin pain test, and completely inhibits paw licking and lifting responses at 10 mg/kg (i.p.)^[4].

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

Animal Model:

BKS.Cg-Dock7m+/+ Leprdb (db/db) (6-week-old male, spontaneous genetic diabetic kidney disease model)^[2]
Dosage:

0.3 mg/kg/day; 1.5 mg/kg/day
Administration:

p.o.; once daily; 4 weeks
Result:

Significantly reduced serum blood urea nitrogen and creatinine levels relative to untreated DKD mice.
Significantly decreased urinary albumin-to-creatinine ratios relative to untreated DKD mice.
Significantly lowered fasting blood glucose and homeostatic model assessment of insulin resistance levels relative to untreated DKD mice.
Significantly reduced renal tubular injury scores and collagen deposition (renal fibrosis) compared to untreated DKD mice.
Significantly attenuated the phosphorylation of JNK, p65, and c-Jun in kidney tissues relative to untreated DKD mice.
Significantly decreased the expression of inflammatory markers (IL-1β, IL-6, TNF-α), apoptotic markers (cleaved caspase-3, cleaved PARP), and fibrotic markers (TGF-β, phospho-Smad2/3, collagen 1) in kidney tissues relative to untreated DKD mice.
Showed no dose-dependent effect between 0.3 mg/kg/day and 1.5 mg/kg/day doses.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 90494-79-4
Appearance Solid
Molecular Weight 417.89
Formula C₂₄H₂₃ClF₃N
Color White to off-white
SMILES

FC(C1=CC(C2=CCN(CCC3=CC=C4C=CC=CC4=C3)CC2)=CC=C1)(F)F.[H]Cl
Synonyms

SR57746A; SR57746 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (1)

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Biochem Pharmacol

Xaliproden improves diabetic kidney disease through JNK-mediated renal tubular protection. [Abstract]

2026 Mar 22:117923. PMID: 41876014

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (79.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3930 mL

11.9649 mL

23.9297 mL

5 mM

0.4786 mL

2.3930 mL

4.7859 mL

10 mM

0.2393 mL

1.1965 mL

2.3930 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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In Vivo:

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

Stock Solution Working Solution

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 (5.98 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.98 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Appert-Collin A, et al. Xaliproden (SR57746A) induces 5-HT1A receptor-mediated MAP kinase activation in PC12 cells. Int J Immunopathol Pharmacol. 2005;18(2):233-244. [Content Brief]

[2]. Lee HJ, et al. Xaliproden improves diabetic kidney disease through JNK-mediated renal tubular protection. Biochem Pharmacol. Published online March 22, 2026. [Content Brief]

[3]. Andoh T, et al. Effects of xaliproden, a 5-HT₁A agonist, on mechanical allodynia caused by chemotherapeutic agents in mice. Eur J Pharmacol. 2013;721(1-3):231-236. [Content Brief]

[4]. Martel JC, et al. 5-HT1A receptors are involved in the effects of xaliproden on G-protein activation, neurotransmitter release and nociception. Br J Pharmacol. 2009;158(1):232-242. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3930 mL	11.9649 mL	23.9297 mL	59.8244 mL
	5 mM	0.4786 mL	2.3930 mL	4.7859 mL	11.9649 mL
	10 mM	0.2393 mL	1.1965 mL	2.3930 mL	5.9824 mL
	15 mM	0.1595 mL	0.7977 mL	1.5953 mL	3.9883 mL
	20 mM	0.1196 mL	0.5982 mL	1.1965 mL	2.9912 mL
	25 mM	0.0957 mL	0.4786 mL	0.9572 mL	2.3930 mL
	30 mM	0.0798 mL	0.3988 mL	0.7977 mL	1.9941 mL
	40 mM	0.0598 mL	0.2991 mL	0.5982 mL	1.4956 mL
	50 mM	0.0479 mL	0.2393 mL	0.4786 mL	1.1965 mL
	60 mM	0.0399 mL	0.1994 mL	0.3988 mL	0.9971 mL

Xaliproden hydrochloride

1 Cited Publications

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Xaliproden hydrochloride

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All 5-HT Receptor Isoforms

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Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Xaliproden hydrochloride Related Classifications

HY-14604 Related Classifications