Paroxetine hydrochloride hemihydrate
Based on 11 publication(s) in Google Scholar
Paroxetine (BRL29060) hydrochloride hemihydrate is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine hydrochloride hemihydrate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine hydrochloride hemihydrate is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine hydrochloride hemihydrate is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 110429-35-1
- Formula: C19H22ClFNO3.5
- Molecular Weight:374.84
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Paroxetine hydrochloride hemihydrate
More- Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]
- Autophagy. 2025 May;21(5):934-956. [Abstract]
- Cell Rep Med. 2026 Jan 20;7(1):102537. [Abstract]
- J Chem Inf Model. 2021 Aug 23;61(8):3804-3813. [Abstract]
- Front Pharmacol. 2024 Jul 31:15:1389761. [Abstract]
- ACS Omega. 2025 Oct 17;10(42):50208-50217. [Abstract]
- Sci Rep. 2025 Oct 21;15(1):36797. [Abstract]
- Brain Res. 2019 Oct 1:1720:146296. [Abstract]
- J Mol Cell Cardiol Plus. 2024 Mar 26:8:100072. [Abstract]
- University of South Carolina. 2025.
- Patent. US20250127769A1.
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
Biological Activity
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GRK2 |
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Cell Line
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Type | Value | Description | References |
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| BTI-TN-5B1-4 | IC50 |
1.38 μM
Compound: Paroxetine
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Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method
Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method
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[PMID: 27050625] |
| CHO | IC50 |
0.56 nM
Compound: Paroxetine
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Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
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[PMID: 27865645] |
| CHO | IC50 |
3.9 μM
Compound: paroxetine
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Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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[PMID: 23812503] |
| HEK293 | IC50 |
0.2 nM
Compound: paroxetine
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Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells after 1 hr by scintillation counting analysis
Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells after 1 hr by scintillation counting analysis
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[PMID: 23477943] |
| U-373MG ATCC | IC50 |
900 nM
Compound: paroxetine
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Displacement of [125I]substance P from human recombinant NK1 receptor expressed in human U373 cells after 1 hr by scintillation counting analysis
Displacement of [125I]substance P from human recombinant NK1 receptor expressed in human U373 cells after 1 hr by scintillation counting analysis
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[PMID: 23477943] |
Paroxetine hydrochloride hemihydrate potently and selectively inhibits serotonin reuptake in rat brain synaptosomes, with a Ki of 1.1 nmol/L, and shows much weaker activity against norepinephrine and dopamine reuptake[1].
Paroxetine hydrochloride hemihydrate has no significant affinity for most tested neurotransmitter receptors in rat brain tissue, only showing weak binding to muscarinic cholinergic receptors with a Ki of 89 nmol/L[1].
Paroxetine hydrochloride hemihydrate (76 nM) exhibits high affinity for the muscarinic M1 receptor, resulting in greater anticholinergic effects than other SSRIs[2].
Paroxetine hydrochloride hemihydrate exhibits estrogenic activity in an in vitro assay that identifies chemicals disrupting aromatase and estrogen balance in humans, which may promote estrogen-sensitive breast tumor growth[2].
Paroxetine hydrochloride hemihydrate (10-20 μM; 6-24 h) differentially modulates LPS-induced cytokine production in Raw264.7 mouse macrophages, potently inhibiting IL-6 production and enhancing TNFα production at 10 μM and 20 μM concentrations after 6 and 24 hours of incubation[3].
Paroxetine hydrochloride hemihydrate (10-20 μM; 6-24 h) differentially modulates LPS-induced cytokine production in thioglycollate-elicited primary mouse peritoneal macrophages, potently inhibiting IL-6 production and enhancing TNFα production at 10 μM and 20 μM concentrations after 6 and 24 hours of incubation[3].
Paroxetine hydrochloride hemihydrate (20 μM; 24 h) inhibits LPS-induced IL-6 production independent of 5-HT2/5-HT7 receptors and enhances LPS-induced TNFα production via 5-HT2/5-HT7 receptors in Raw264.7 mouse macrophages after 24 hours of incubation[3].
Paroxetine hydrochloride hemihydrate (20 μM) modulates LPS-induced IL-6 and TNFα production in Raw264.7 mouse macrophages independently of GRK2, as its inhibitory effect on IL-6 and enhancing effect on TNFα are retained in GRK2-knockdown cells[3].
Paroxetine hydrochloride hemihydrate (10-30 μM, 72 h) reduces the viability of MCF-7 cells in a time- and dose-dependent manner[4].
Paroxetine hydrochloride hemihydrate (10-30 μM, 1-12 h) induces mitochondrial-mediated apoptosis in MCF-7, increasing ROS generation[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Raw264.7 mouse macrophages
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Concentration:10 μM; 20 μM
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Incubation Time:6 h; 24 h
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Result:Reduced LPS-induced IL-6 production to ~75% of LPS-only levels at 6 hours with 10 μM.
Reduced LPS-induced IL-6 production to ~50% of LPS-only levels at 6 hours with 20 μM.
Reduced LPS-induced IL-6 production to ~80% of LPS-only levels at 24 hours with 10 μM.
Reduced LPS-induced IL-6 production to ~60% of LPS-only levels at 24 hours with 20 μM.
Increased LPS-induced TNFα production to ~155% of LPS-only levels at 6 hours with 10 μM.
Increased LPS-induced TNFα production to ~195% of LPS-only levels at 6 hours with 20 μM.
Increased LPS-induced TNFα production to ~120% of LPS-only levels at 24 hours with 10 μM.
Increased LPS-induced TNFα production to ~145% of LPS-only levels at 24 hours with 20 μM.
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Cell Line:Raw264.7 mouse macrophages pretreated with 5-HT2/5-HT7 receptor antagonist LY215840
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Concentration:20 μM
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Incubation Time:24 h
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Result:Reduced LPS-induced IL-6 production to ~45% of LPS-only levels.
Increased LPS-induced TNFα production to ~180% of LPS-only levels.
Co-treatment with LY215840 (10 nM, 100 nM, 1 μM) further reduced IL-6 levels to below ~20% of LPS-only levels.
Co-treatment with LY215840 (10 nM, 100 nM, 1 μM) reversed TNFα enhancement, reducing levels to ~80%, ~40%, and ~40% of LPS-only levels, respectively (for 100 nM and 1 μM LY215840).
Paroxetine hydrochloride hemihydrate exerts no significant dopaminergic, sedative, or ethanol-potentiating effects in healthy rodent models[1].
Paroxetine hydrochloride hemihydrate produces extremely mild cardiovascular effects in healthy cats, rabbits, and dogs compared with tricyclic antidepressants, and exhibits weak quinidine-like activity only at serotonin reuptake-blocking doses[1].
Combination of Paroxetine hydrochloride hemihydrate with monoamine oxidase inhibitors (MAOIs) or serotonin precursors induces serotonin syndrome in rats[1].
Paroxetine hydrochloride hemihydrate modulates the hypothalamic-pituitary-adrenal axis and prolactin-related endocrine activity in healthy rats[1].
Acute treatment with Paroxetine (5 mg/kg) hydrochloride hemihydrate increases extracellular serotonin levels in the brain of healthy rats[1].
Paroxetine hydrochloride hemihydrate antagonizes apomorphine-induced hypothermia in rats, indicating that it exhibits noradrenergic activity at high doses[1].
Combination treatment with Paroxetine hydrochloride hemihydrate (for 3 consecutive weeks) and Pravastatin (HY-B0165) increases the blood glucose level of prediabetic, insulin-resistant mice from 128 mg/dl to 193 mg/dl[2].
Paroxetine (10 mg/kg, i.p., once a day for 14 days) hydrochloride hemihydrate reduces neurogenic pain in rats both before and after sciatic nerve injury[5].
Paroxetine (0.3-10 mg/kg, orally, single dose) hydrochloride hemihydrate has anti-anxiety and antidepressant effects in rats, increasing social interaction time[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[6]
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Dosage:0.3, 1, 3, 10 mg/kg; single dose
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Administration:p.o.
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Result:Reduced the synthesis rate of serotonin and increased the social time of rats, but had no effect on motor activity. The motor activity of animals taking the drug for a long time was slightly lower than that of animals taking the drug for a short time.
Chemical Information
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CAS No. 110429-35-1
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Appearance Solid
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Molecular Weight 374.84
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Formula C19H22ClFNO3.5
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Color White to off-white
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SMILES
FC(C=C1)=CC=C1[C@H](CCNC2)[C@@H]2COC3=CC=C(OCO4)C4=C3.Cl.[0.5H2O]
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Synonyms
BRL29060 hydrochloride hemihydrate; BRL29060A hemihydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (11)
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Journal Impact Factor
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Most Recent
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Cell
2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809 -
Autophagy
2025 May;21(5):934-956. PMID: 39663580 -
Cell Rep Med
5-HT reuptake blockade induces pyroptosis in BRAFV600E-mutated melanomas via remodeling histone serotonylation. [Abstract]2026 Jan 20;7(1):102537. PMID: 41494533
Paroxetine hydrochloride hemihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102537. [Abstract]
IC50 of Paroxetine hydrochloride (1-12.5 μM) in the indicated cell lines.
Paroxetine hydrochloride hemihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102537. [Abstract]
Colony formation assays in the indicated cells treated with DMSO or gradient doses of Paroxetine hydrochloride (0.5-7.5 μM).
Paroxetine hydrochloride hemihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102537. [Abstract]
A375 xenografts were established and treated with vehicle or Paroxetine hydrochloride (25 mg/kg daily intraperitoneally [i.p.]) for 14 days. Tumors in each group were individually recorded every 2 days. n = 8 tumors per group.
Paroxetine hydrochloride hemihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102537. [Abstract]
5-HT levels in A375 cells treated with DMSO or the indicated Paroxetine hydrochloride treatment for 24 h.
Paroxetine hydrochloride hemihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102537. [Abstract]
A375DTR xenografts were established and treated with vehicle or PH (25 mg/kg daily i.p. injection) for 15 days. The tumors in each group were individually recorded every 3 days. n = 8 tumors per group.
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J Chem Inf Model
Development of Machine Learning Models and the Discovery of a New Antiviral Compound against Yellow Fever Virus. [Abstract]2021 Aug 23;61(8):3804-3813. PMID: 34286575 -
Front Pharmacol
N-demethylsinomenine metabolite and its prototype sinomenine activate mast cells via MRGPRX2 and aggravate anaphylaxis. [Abstract]2024 Jul 31:15:1389761. PMID: 39144634 -
ACS Omega
2025 Oct 17;10(42):50208-50217. PMID: 41179162 -
Sci Rep
Paroxetine suppresses 27-hydroxycholesterol-induced responses in THP-1 human monocytic cells by regulating the AKT/mTORC1 pathway. [Abstract]2025 Oct 21;15(1):36797. PMID: 41120475 -
Brain Res
Serum miR-221-3p as a new potential biomarker for depressed mood in perioperative patients. [Abstract]2019 Oct 1:1720:146296. PMID: 31211948
Paroxetine hydrochloride hemihydrate purchased from MedChemExpress. Usage Cited in: Brain Res. 2019 Oct 1:1720:146296. [Abstract]
Protein levels of IFNα and IRF2(B) are detected in HA1800 Cells at 6 h, 12 h and 24 h after paroxetine (10μM) treatment by RT-qPCR and western blot respectively.
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J Mol Cell Cardiol Plus
The selective serotonin reuptake inhibitor paroxetine improves right ventricular systolic function in experimental pulmonary hypertension. [Abstract]2024 Mar 26:8:100072. PMID: 39802918 -
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Solvent & Solubility
DMSO : 100 mg/mL (266.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.34 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.34 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (288 KB)
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SDS (598 KB)
- English - EN (598 KB)
- Français - FR (598 KB)
- Deutsch - DE (598 KB)
- Norwegian - NO (598 KB)
- Español - ES (598 KB)
- Swedish - SV (598 KB)
- Italian - IT (598 KB)
- Korean - KR (598 KB)
- Portuguese - PT (598 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang Q, et al. Paroxetine alleviates T lymphocyte activation and infiltration to joints of collagen-induced arthritis. Sci Rep. 2017 Mar 28;7:45364. [Content Brief]
[2]. Liu RP, et al. Paroxetine ameliorates lipopolysaccharide-induced microglia activation via differential regulation of MAPK signaling. J Neuroinflammation. 2014 Mar 12;11:47. [Content Brief]
[3]. Lassen TR, et al. Effect of paroxetine on left ventricular remodeling in an in vivo rat model of myocardial infarction. Basic Res Cardiol. 2017 May;112(3):26. [Content Brief]
[4]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069. [Content Brief]
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, 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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6678 mL | 13.3390 mL | 26.6780 mL | 66.6951 mL |
| 5 mM | 0.5336 mL | 2.6678 mL | 5.3356 mL | 13.3390 mL | |
| 10 mM | 0.2668 mL | 1.3339 mL | 2.6678 mL | 6.6695 mL | |
| 15 mM | 0.1779 mL | 0.8893 mL | 1.7785 mL | 4.4463 mL | |
| 20 mM | 0.1334 mL | 0.6670 mL | 1.3339 mL | 3.3348 mL | |
| 25 mM | 0.1067 mL | 0.5336 mL | 1.0671 mL | 2.6678 mL | |
| 30 mM | 0.0889 mL | 0.4446 mL | 0.8893 mL | 2.2232 mL | |
| 40 mM | 0.0667 mL | 0.3335 mL | 0.6670 mL | 1.6674 mL | |
| 50 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3339 mL | |
| 60 mM | 0.0445 mL | 0.2223 mL | 0.4446 mL | 1.1116 mL | |
| 80 mM | 0.0333 mL | 0.1667 mL | 0.3335 mL | 0.8337 mL | |
| 100 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL |
- Paroxetine hydrochloride hemihydrate
- 110429-35-1
- BRL29060 hydrochloride hemihydrate
- BRL29060A hemihydrate
- Autophagy
- G Protein-coupled Receptor Kinase (GRK)
- Serotonin Transporter
- 5-HT2 receptors
- Raw264.7 mouse macrophages
- nitric oxide synthase
- 5-HT1B/1D autoreceptors
- serotonin reuptake transporter
- cytochrome P450 3A4
- 5-HT1A autoreceptor
- norepinephrine reuptake transporter
- cytochrome P450 2D6
- muscarinic cholinergic receptor
- Inhibitor
- inhibitor
- inhibit