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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- No. CAS: 1081317-31-8
- Fòrmula: C36H37N3O2
- Peso molecular:543.70
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Actividad biológica
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Nav1.7 |
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 (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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No. CAS 1081317-31-8
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Peso molecular 543.70
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DA-0218 Related Classifications
HY-182710 Related Classifications
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