2. Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation MAPK/ERK Pathway NF-κB
  3. Cholinesterase (ChE) Potassium Channel Amyloid-β TRP Channel Tau Protein NOD-like Receptor (NLR) JNK NF-κB IKK
  4. Drofenine hydrochloride

Drofenine hydrochloride  (Synonyms: Hexahydroadiphenine hydrochloride)

Cat. No.: HY-B1239 Purity: 98.0%
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Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.

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

Drofenine hydrochloride

Drofenine hydrochloride Chemical Structure

CAS No. : 548-66-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Drofenine hydrochloride:

Drofenine hydrochloride Related Antibodies

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1 Publications Citing Use of MCE Drofenine hydrochloride

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IKK-α IKK-β IKK IKKε TBK1

  • Biological Activity

  • Purity & Documentation

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Description

Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm[1][2][3][4].

IC50 & Target[1]

BChE

3 μM ()

KV2.1

9.53 μM ()

TRPV3

 

NLRP3

 

In Vitro

Drofenine (10 μM; 0.5 h) hydrochloride suppresses oligomeric Aβ (o-Aβ)-enhanced Kv2.1-dependent outward potassium current and density in CHO-Kv2.1 cells by blocking o-Aβ-induced delays in Kv2.1 channel inactivation[1].
Drofenine (5-20 μM; 30 min) hydrochloride inhibits membrane potential in CHO-Kv2.1 cells without affecting normal CHO cells[2].
Drofenine (5-20 μM) hydrochloride does not reduce the viability of CHO-Kv2.1 cells[2].
Drofenine (1-10 μM) hydrochloride potently inhibits Kv2.1 channel currents in CHO-Kv2.1 cells with an IC50 of 9.53 μM[2].
Drofenine (1-10 μM) hydrochloride shows minimal inhibition of Kv2.2 channel currents in CHO-Kv2.2 cells at concentrations that effectively inhibit Kv2.1, indicating selectivity for Kv2.1[2].
Drofenine (0.01-0.1 mM) hydrochloride acts as a pure competitive inhibitor of purified human serum butyrylcholinesterase, with a Ki value of 0.003 mM[3].
Drofenine (30-1000 μM) hydrochloride acts as a selective agonist of human TRPV3 in TRPV3-overexpressing HEK-293 cells, activating calcium flux with an EC50 of 207 μM without activating TRPA1, TRPM8, TRPV1, TRPV2, or TRPV4 at concentrations up to 1000 μM[4].
Drofenine (30-1000 μM) hydrochloride acts as a potent agonist of endogenous TRPV3 in HaCaT human keratinocytes, inducing calcium flux with an EC50 of 605 μM[4].
Drofenine (10-1000 μM; 24 h) hydrochloride is cytotoxic to HaCaT human keratinocytes after 24 h of incubation, with an LC50 of 230 μM[4].

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

Drofenine hydrochloride Related Antibodies

Cell Viability Assay[4].

Cell Line: human immortalized keratinocyte (HaCaT) cells
Concentration: 10-1000 μM
Incubation Time: 24 h
Result: Was more cytotoxic to HaCaT cells than 2-APB and carvacrol, with an LC50 of 230 μM, compared to LC50 values of >300 μmol/L for both 2-APB (HY-W009724) and carvacrol (HY-N0711).
In Vivo

Drofenine (10 mg/kg/day; i.p.; daily; 8 weeks) hydrochloride ameliorates cognitive impairment, neuroinflammation, tauopathy, synaptic dysfunction, and neuronal loss in 5xFAD Alzheimer's disease mice by inhibiting the Kv2.1/JNK/NF-κB pathway, with no observable hepatotoxicity or nephrotoxicity[1].
Drofenine (10-20 mg/kg; 4 total doses; Weeks 7, 8, 9, 10 post-STZ injection) hydrochloride suppresses Kv2.1 expression and function in DRG tissue, promotes DRG neuron neurite outgrowth, and ameliorates motor and sensory deficits in STZ (HY-13753)-induced type 1 DPN mice via Kv2.1 inhibition[2].
Drofenine (10-20 mg/kg; 4 total doses; Weeks 1, 2, 3, 4 of study period) hydrochloride suppresses Kv2.1 expression and function in DRG tissue, promotes DRG neuron neurite outgrowth, and ameliorates motor and sensory deficits in spontaneous type 2 db/db DPN mice[2].

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

Animal Model: 5xFAD transgenic (APPSwFlLon, PSEN1-M146L-L286V) (female, 7 months old at treatment start, Alzheimer's disease model); wild-type (WT) (female)[1]
Dosage: 10 mg/kg/day
Administration: i.p.; daily; 8 weeks
Result: Improved short-term working memory via increased discrimination index in novel object recognition test.
Improved spatial working memory via increased number of novel arm crossings in Y-maze test.
Improved spatial learning and long-term memory via reduced escape latency in Morris water maze training trials and increased platform crossing frequency in Morris water maze probe trials in 5xFAD mice; no cognitive improvement observed in Kv2.1-knockdown 5xFAD mice.
Reduced Iba1-positive microglial and GFAP-positive astrocytic gliosis in 5xFAD mouse brains.
Reduced NLRP3-ASC positive puncta, and reduced protein levels of NLRP3, p-NLRP3, ASC, Cas1 (p20), IL-1β, p-JNK, and p-NF-κB in 5xFAD mice.
Reduced microglial NF-κB nuclear translocation in 5xFAD mice; no anti-inflammatory effects observed in Kv2.1-knockdown 5xFAD mice.
Reduced AT8-positive hyperphosphorylated Tau (Ser202/Thr205) areas in the hippocampus of 5xFAD mice.
Reduced protein levels of p396-Tau, p231-Tau, p199-Tau, p-GSK3β, and p-CaMKII-α in 5xFAD mice; no effects on Tau phosphorylation or related kinases observed in Kv2.1-knockdown 5xFAD mice.
Improved long-term potentiation induction and maintenance in the hippocampal DG region of 5xFAD mice.
Restored protein levels of synaptic markers PSD95, synaptophysin (SYN), and VAMP2 in 5xFAD mice; no synaptic improvement observed in Kv2.1-knockdown 5xFAD mice.
Reduced TUNEL-positive apoptotic neurons in 5xFAD mice.
Reversed loosely arranged neuronal nuclei (Nissl staining) in the hippocampus of 5xFAD mice; no effects on neuronal survival observed in Kv2.1-knockdown 5xFAD mice.
Showed no significant hepatotoxicity or nephrotoxicity via no changes in serum ALT, AST, or urea levels in treated WT or 5xFAD mice.
Animal Model: C57BL/6 (male, 7 weeks old at study initiation, streptozotocin-induced type 1 diabetes)[2]
Dosage: 10 mg/kg; 20 mg/kg
Administration: 4 total doses; Weeks 7, 8, 9, 10 post-STZ injection
Result: Lowered Kv2.1/T-ERK ratios relative to vehicle-treated STZ mice.
Decreased relative Kv2.1 area in DRG tissue compared to vehicle-treated STZ mice.
Lowered relative Kv2.1 mRNA levels compared to vehicle-treated STZ mice.
Reduced elevated potassium currents in STZ mouse DRG neurons.
Increased total neurite length relative to vehicle-treated STZ mice.
Improved motor nerve conduction velocity relative to vehicle-treated STZ mice.
Reduced sensitivity to mechanical stimuli relative to vehicle-treated STZ mice.
Normalized thermal response relative to vehicle-treated STZ mice.
Animal Model: BKS Cg-m+/+Leprdb/J (db/db) (male, 17 weeks old at study initiation, spontaneous type 2 diabetes)[2]
Dosage: 10 mg/kg; 20 mg/kg
Administration: 4 total doses; Weeks 1, 2, 3, 4 of study period
Result: Lowered Kv2.1/T-ERK ratios relative to vehicle-treated db/db mice.
Decreased relative Kv2.1 area in DRG tissue compared to vehicle-treated db/db mice.
Lowered relative Kv2.1 mRNA levels compared to vehicle-treated db/db mice.
Reduced elevated potassium currents at +50 mV in db/db mouse DRG neurons.
Increased total neurite length relative to vehicle-treated db/db mice.
Improved motor nerve conduction velocity relative to vehicle-treated db/db mice.
Reduced sensitivity to mechanical stimuli relative to vehicle-treated db/db mice.
Normalized thermal response relative to vehicle-treated db/db mice.
Molecular Weight

353.93

Formula

C20H32ClNO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCCN(CC)CC)C(C1CCCCC1)C2=CC=CC=C2.[H]Cl
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)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 75 mg/mL (211.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 33.3 mg/mL (94.09 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8254 mL 14.1271 mL 28.2542 mL
5 mM 0.5651 mL 2.8254 mL 5.6508 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, 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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

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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 (7.06 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 (7.06 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 16.67 mg/mL (47.10 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 98.10%

SDS (761 KB)

COA (248 KB) HNMR (191 KB) LCMS (389 KB)

Handling Instructions (2659 KB)
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, 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
H2O / DMSO 1 mM 2.8254 mL 14.1271 mL 28.2542 mL 70.6354 mL
5 mM 0.5651 mL 2.8254 mL 5.6508 mL 14.1271 mL
10 mM 0.2825 mL 1.4127 mL 2.8254 mL 7.0635 mL
15 mM 0.1884 mL 0.9418 mL 1.8836 mL 4.7090 mL
20 mM 0.1413 mL 0.7064 mL 1.4127 mL 3.5318 mL
25 mM 0.1130 mL 0.5651 mL 1.1302 mL 2.8254 mL
30 mM 0.0942 mL 0.4709 mL 0.9418 mL 2.3545 mL
40 mM 0.0706 mL 0.3532 mL 0.7064 mL 1.7659 mL
50 mM 0.0565 mL 0.2825 mL 0.5651 mL 1.4127 mL
60 mM 0.0471 mL 0.2355 mL 0.4709 mL 1.1773 mL
80 mM 0.0353 mL 0.1766 mL 0.3532 mL 0.8829 mL
DMSO 100 mM 0.0283 mL 0.1413 mL 0.2825 mL 0.7064 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Keywords:

Drofenine548-66-3HexahydroadiphenineCholinesterase (ChE)Potassium ChannelAmyloid-βTRP ChannelTau ProteinNOD-like Receptor (NLR)JNKNF-κBIKKKcsAβ-amyloid peptideAβAbetaTransient receptor potential channelsc-Jun N-terminal kinaseNuclear factor-κBNuclear factor-kappaBIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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