DD-161515
DD-161515 is a TRPV1/VR1 inhibitor with an IC50 of 0.7 μM in rats. DD-161515 binds to an allosteric site of TRPV1 distinct from that of capsaicin, blocks channel opening, inhibits receptor-mediated calcium ion influx, reduces the excitability of peripheral sensory nerve fibers, and thereby inhibits nociception induced by heat and transmission of chemically induced pain signals. DD-161515 can be used in studies related to inflammatory pain.
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- No. CAS: 410080-55-6
- Fòrmula: C29H37Cl4N5O3
- Peso molecular:645.45
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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rTRPV1 0.7 μM (IC50) |
DD-161515 preferentially inhibits TRPV1 channel activity with micromolar potency and moderate voltage-dependency[1].
DD-161515 acts as a potent, noncompetitive antagonist of recombinant rat VR1 channels expressed in Xenopus oocytes, with an IC50 of 0.7 μM[2].
DD-161515 inhibits capsaicin-evoked Ca2+ influx in ~70% of cultured newborn mouse trigeminal primary sensory neurons by ≥ 90% at 100 μM, with reversible blockade[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DD-161515 (0.05-0.2 mmol/kg; i.p.; single administration) dose-dependently abolishes capsaicin-induced pain behaviors and prevents neurogenic inflammation[2].
DD-161515 (0.4 μmol; intra-arterial administration; single dose) reversibly inhibits capsaicin-induced activation of knee joint nociceptor fibers[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (adult male)[2]
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Dosage:0.05 mmol/kg; 0.1 mmol/kg; 0.2 mmol/kg
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Administration:i.p.; single dose
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Result:Increased latency to first pain behavior 13-fold to 269 s at 0.2 mmol/kg compared to vehicle latency of 20 s, and reduced pain behavior duration to near zero.
Increased latency to first pain behavior to 80 s at 0.05 mmol/kg.
Prevented capsaicin-induced ipsilateral paw volume increase at 0.05 mmol/kg and 0.2 mmol/kg, with ipsilateral paw volumes measuring 15.3 mm3 and 15.2 mm3 respectively, compared to vehicle-treated mice where ipsilateral paw volume was 20.6 mm3.
Chemical Information
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No. CAS 410080-55-6
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Peso molecular 645.45
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Fòrmula C29H37Cl4N5O3
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SMILES
O=C(CN(CCC1=CC=C(C=C1Cl)Cl)C(CN(CCC2=CC=C(C=C2Cl)Cl)C(CNCCC3N(CCC3)C)=O)=O)N
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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)
DD-161515 Related Classifications
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