TrkA-IN-23
TrkA-IN-23 is an allosteric, orally active, selective TrkA inhibitor with an IC50 of 4 nM. TrkA-IN-23 inhibits NGF-induced phosphorylated ERK formation. TrkA-IN-23 reverses thermal hyperalgesia and eliminates Capsaicin (HY-10448) sensitization in NGF-sensitized skin. TrkA-IN-23 can be used for research on inflammatory diseases.
For research use only. We do not sell to patients.
- CAS No.: 1821484-84-7
- Formula: C26H23Cl2N5O3
- Molecular Weight:524.40
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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]|
TrkA 4 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.23 μM
Compound: 3
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Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 34871843] |
In Vitro
TrkA-IN-23 binds non-activated unphosphorylated TrkA with a KD of 4.2 nM[1].
TrkA-IN-23 (10 μM) exhibits high selectivity for TrkA in biochemical and cellular assays covering 392 kinases, and displays a clean off-target profile across 84 Cerep targets[1].
TrkA-IN-23 inhibits TrkA in PathHunter cells with an IC50 of 10 nM, showing 180-fold selectivity over TrkB and 70-fold selectivity over TrkC[1].
TrkA-IN-23 inhibits NGF-induced formation of phosphorylated ERK in native adult rat DRG with an IC50 of approximately 57 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat UVIH inflammatory pain model[1]
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Dosage:1.2 mg/kg; 12 mg/kg; 40 mg/kg
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Administration:p.o.; single dose; 48 h after UV exposure
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Result:Thermal hyperalgesia was reversed at doses of 12 and 40 mg/kg at each of the 1, 3, and 6 h time-points studied.
No effect was seen with any dose on thermal withdrawal response on the contralateral hindpaw.
Chemical Information
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CAS No. 1821484-84-7
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Molecular Weight 524.40
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Formula C26H23Cl2N5O3
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SMILES
O=C(NCC(O)(C)C)C1=NN(C=2C=CC=CC2)C(=C1)NC(=O)C3=CC(=C(Cl)C=C3Cl)C4=NC=CC=C4
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TrkA-IN-23 Related Classifications
HY-115485 Related Classifications
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