Cat. No.: HY-B1239

Drofenine hydrochloride

(Synonyms: Hexahydroadiphenine hydrochloride)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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 K_i 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.

Purity: 98.0%
CAS No.: 548-66-3
Formula: C₂₀H₃₂ClNO₂
Molecular Weight:353.93

Storage:

4°C, sealed storage, away from moisture

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

Drofenine hydrochloride Chemical Structure

CAS No.: 548-66-3

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

Biological Activity

Description

IC₅₀ & Target^[1]

BChE

3 μM ()

KV2.1

9.53 μM ()

TRPV3

NLRP3

All Cholinesterase (ChE) Isoforms :

AChE
BChE

All TRP Channel Isoforms :

All NOD-like Receptor (NLR) Isoforms :

All JNK Isoforms :

All NF-κB Isoforms :

All IKK Isoforms :

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 K_i 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.

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.

Chemical Information

CAS No. 548-66-3
Appearance Solid
Molecular Weight 353.93
Formula C₂₀H₃₂ClNO₂
Color White to off-white
SMILES

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

Hexahydroadiphenine 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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Journal Impact Factor

Biochem Biophys Res Commun

Inhibition of the transient receptor potential vanilloid 3 channel attenuates carbon tetrachloride-induced hepatic fibrosis. [Abstract]

2021 Jun 18:558:86-93. PMID: 33906111

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8254 mL

14.1271 mL

28.2542 mL

5 mM

0.5651 mL

2.8254 mL

5.6508 mL

10 mM

0.2825 mL

1.4127 mL

2.8254 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.

* 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.

Molarity Calculator

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

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Molecular Weight Molecular Weight

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 (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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (7.06 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.

Working Solution

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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.

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (298 KB)
SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Korean - KR (761 KB)
- Portuguese - PT (761 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]. Lu J, et al. Drofenine as a Kv2.1 inhibitor alleviated AD-like pathology in mice through Aβ/Kv2.1/microglial NLRP3/neuronal Tau axis. Acta Pharm Sin B. 2025;15(1):371-391. [Content Brief]

[2]. Xu X, et al. Antispasmodic Drug Drofenine as an Inhibitor of Kv2.1 Channel Ameliorates Peripheral Neuropathy in Diabetic Mice. iScience. 2020;23(10):101617. Published 2020 Sep 28. [Content Brief]

[3]. Bodur E, et al. Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. Arch Biochem Biophys. 2001 Feb 1;386(1):25-29. [Content Brief]

[4]. Deering‐Rice C E, et al. Drofenine: a 2‐APB analog with improved selectivity for human TRPV3[J]. Pharmacology research & perspectives, 2014, 2(5): e00062. [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
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.

Keywords

Drofenine hydrochloride

1 Cited Publications

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Drofenine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Drofenine hydrochloride

All Cholinesterase (ChE) Isoforms

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All IKK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Drofenine hydrochloride Related Classifications

HY-B1239 Related Classifications