2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. DA-0218

DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus.

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DA-0218

DA-0218 Chemical Structure

CAS No. : 1081317-31-8

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DA-0218 Related Antibodies

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Description

DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus[1][2].

IC50 & Target[1]

Nav1.7

 

In Vitro

DA-0218 (Compound 9) (0.01-10 μM; 14 min) potently inhibits Nav1.7-mediated sodium currents in HEK293 cells expressing Nav1.7, with an IC50 of 0.74 μM, and shows no activity against HEK293 cells expressing Nav1.5[1].
DA-0218 (10 μM) exerts a moderate inhibitory effect on transient sodium currents in human DRG neurons, reducing the peak current by 22% at 10 μM[1].
DA-0218 (10 μM; up to 14 min incubation and recording) inhibits the peak transient sodium current by 44% in small-diameter mouse dorsal root ganglion neurons pretreated with Paclitaxel (HY-B0015)[2].
DA-0218 (10 μM; up to 14 min incubation and recording) inhibits the peak transient sodium current of small-diameter human dorsal root ganglion neurons by 22%[2].

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

DA-0218 Related Antibodies
In Vivo

DA-0218 (intrathecal injection at 3-30 nM; intraperitoneal injection at 30 mg/kg; plantar injection at 60 nM; single administration) potently inhibits formalin-induced inflammatory pain in mice, achieving up to 80% relief of phase II pain at the highest intrathecal dose[2].
DA-0218 (10-30 nM; intrathecal injection; 10-30 mg/kg; intraperitoneal injection; single administration) transiently reverses paclitaxel-induced mechanical hyperalgesia in mice, but repeated administration leads to acute tolerance, and intraperitoneal administration shows no effect[2].
DA-0218 (intrathecal injection, 3-30 nM) inhibits Histamine (HY-B1204)-induced acute pruritus in mice[2].
DA-0218 (intrathecal injection, 30 nM) potently inhibits chronic pruritus induced by mouse lymphoma, with a duration of action of at least 5 h[2].

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

Animal Model: C57BL/6 (male and female; formalin-induced inflammatory pain model)[2]
Dosage: 3; 10; 30 nM (i.t.); 30 mg/kg (i.p.); 60 nM (i.pl.)
Administration: i.t.; i.p.; i.pl.; single administration
Result: Produced dose-dependent inhibition of formalin-induced phase II pain by up to 80%.
Reduced phase I pain at the 30 nmol i.t. dose.
Inhibited phase II pain by 76% at 30 mg/kg i.p..
Significantly reduced phase II pain at 60 nmol i.pl..
Animal Model: C57BL/6 (male and female; paclitaxel-induced neuropathic pain model)[2]
Dosage: 10; 20 ; 30 nM (i.t.); 10; 30 mg/kg (i.p.)
Administration: i.t.; i.p.; single administration
Result: Transiently but completely reversed paclitaxel-induced mechanical allodynia at 1 h and 3 h post-injection in a dose-dependent manner.
Showed no effect on mechanical allodynia at 5 h post-injection.
Resulted in acute tolerance after repeated intrathecal injections of 20 nmol, with no analgesic effect after the second and third injections.
Had no effect on mechanical allodynia at 10 mg/kg and 30 mg/kg i.p..
Animal Model: C57BL/6 (male and female; histamine-induced acute itch model)[2]
Dosage: 3; 10 ; 30 nM
Administration: i.t.; single administration
Result: Produced a dose-dependent reduction in histamine-induced scratch bouts.
Resulted in a statistically significant reduction in total scratches over 30 min at the 30 nmol dose compared to vehicle.
Animal Model: NOD.CB-17-Prkdcscid (male; 8 to 10 weeks old; lymphoma-induced chronic itch model)[2]
Dosage: 30 nM (i.t.)
Administration: i.t.; single administration
Result: Produced a profound reduction in lymphoma-induced chronic scratch bouts at 1 h, 3 h, and 5 h post-injection.
Maintained statistically significant effects through 5 h post-injection.
Molecular Weight

543.70

Formula

C36H37N3O2
CAS No.
SMILES

O=C(NCCN1CCCC1)CC(C2=CC=CC(OC3=CC=CC=C3)=C2)C4=CN(CC5=CC=CC=C5)C6=C4C=CC=C6
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DA-0218 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DA-02181081317-31-8DA0218DA 0218Sodium ChannelNa channelsNa+ channelschronic itchneuropathic painhuman DRG neuronsinflammatory painNav1.5paclitaxel-pretreated neuronsHEK293 cellsacute itchdorsal root ganglion neuronsNav1.7Inhibitorinhibitorinhibit

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