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

Drofenine  (Synonyms: Cycloadiphene; Hexahydroadiphenine)

製品番号: HY-B1239A
取扱説明書 Technical Support

Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine 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 induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.

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Drofenine

Drofenine 構造式

CAS 番号 : 1679-76-1

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Drofenine 関連抗体

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Cholinesterase (ChE) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
AChE BChE

TRP Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
NLRP3 NLRP1 NOD1 NOD2

JNK アイソフォーム固有の製品をすべて表示:

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JNK1 JNK2 JNK3 JNK

NF-κB アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

IKK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
IKK-α IKK-β IKK IKKε TBK1

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製品説明

Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine 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 induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm[1][2][3][4].

IC50 & Target[1]

KV2.1

9.53 μM ()

BChE

3 μM ()

TRPV3

 

NLRP3

 

体外実験

Drofenine (10 μM; 0.5 h) 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) inhibits membrane potential in CHO-Kv2.1 cells without affecting normal CHO cells[2].
Drofenine (5-20 μM) does not reduce the viability of CHO-Kv2.1 cells[2].
Drofenine (1-10 μM) potently inhibits Kv2.1 channel currents in CHO-Kv2.1 cells with an IC50 of 9.53 μM[2].
Drofenine (1-10 μM) 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) acts as a pure competitive inhibitor of purified human serum butyrylcholinesterase, with a Ki value of 0.003 mM[3].
Drofenine (30-1000 μM) 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) 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) 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 関連抗体

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).
体内実験

Drofenine (10 mg/kg/day; i.p.; daily; 8 weeks) 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) 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) 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.
分子量

317.47

分子式

C20H31NO2
CAS 番号
SMILES

O=C(OCCN(CC)CC)C(C1CCCCC1)C2=CC=CC=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

Drofenine1679-76-1Cycloadiphene HexahydroadipheninePotassium ChannelCholinesterase (ChE)TRP ChannelNOD-like Receptor (NLR)Amyloid-βTau ProteinJNKNF-κBIKKKcsATransient receptor potential channelsβ-amyloid peptideAβAbetac-Jun N-terminal kinaseNuclear factor-κBNuclear factor-kappaBIκB kinaseI kappa B kinaseNLRP3 inflammasomeTRPV3human serum butyrylcholinesterase5xFAD Alzheimer's disease miceKv2.1 channelM1/M2 muscarinic receptorsTau hyperphosphorylationHEK-293 cellsHaCaT human keratinocytesCHO-Kv2.1 cellsInhibitorinhibitorinhibit

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