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BMT-090605 

Cat. No.: HY-101290
Handling Instructions

BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively.

For research use only. We do not sell to patients.

BMT-090605 Chemical Structure

BMT-090605 Chemical Structure

CAS No. : 1551403-51-0

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Description

BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1].

In Vitro

BMT-090605 shows a cellular IC50 of 0.63 ±0.39 nM for AAK1[1].

In Vivo

BMT-090605 (0.3-3 µg/rat; intrathecally at lumbar level L5/L6) causes antinociception by inhibiting AAK1 in the spinal cord[1].
The high dose of BMT-090605 (3 µg/rat) showed efficacy comparable to intrathecal clonidine (3 µg/rat). Exposure measurements from this study indicated that brain and plasma levels of BMT-090605 were <4 nM, whereas measurable levels (90–317 nM) were observed in lumbar spinal cord[1].

Animal Model: Male Sprague-Dawley rats (chronic constriction injury (CCI) model)[1]
Dosage: 0.3-3 µg/rat
Administration: Intrathecally at lumbar level L5/L6
Result: Caused a dose-dependent reduction in thermal hyperalgesia.
Molecular Weight

364.44

Formula

C₂₁H₂₄N₄O₂

CAS No.

1551403-51-0

SMILES

N#CC1=C(OC[[email protected]@H](N)CC(C)C)C=C(C(C2=CC=NC(C)=C32)=C1)N(C)C3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BMT-090605BMT090605BMT 090605OthersneuropathicpainchronicconstrictioninjuryCCIBIKEGAKInhibitorinhibitorinhibit

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BMT-090605
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HY-101290
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