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.
For research use only. We do not sell to patients.
- CAS No.: 1081317-31-8
- Formula: C36H37N3O2
- Molecular Weight:543.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
In Vivo
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.
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Animal Model:C57BL/6 (male and female; formalin-induced inflammatory pain model)[2]
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Dosage:3; 10; 30 nM (i.t.); 30 mg/kg (i.p.); 60 nM (i.pl.)
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Administration:i.t.; i.p.; i.pl.; single administration
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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..
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Animal Model:C57BL/6 (male and female; paclitaxel-induced neuropathic pain model)[2]
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Dosage:10; 20 ; 30 nM (i.t.); 10; 30 mg/kg (i.p.)
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Administration:i.t.; i.p.; single administration
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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..
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Animal Model:C57BL/6 (male and female; histamine-induced acute itch model)[2]
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Dosage:3; 10 ; 30 nM
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Administration:i.t.; single administration
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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.
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Animal Model:NOD.CB-17-Prkdcscid (male; 8 to 10 weeks old; lymphoma-induced chronic itch model)[2]
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Dosage:30 nM (i.t.)
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Administration:i.t.; single administration
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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.
Chemical Information
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CAS No. 1081317-31-8
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Molecular Weight 543.70
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Formula C36H37N3O2
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DA-0218 Related Classifications
HY-182710 Related Classifications
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