SARM1-IN-10
SARM1-IN-10 is an orally active SARM1 inhibitor with a pIC50 of 7.1 and a pKd of 8.3. As a base-exchange inhibitor, SARM1-IN-10 forms a NAD+ adduct at the active site of the TIR domain of SARM1, blocks enzymatic function, and induces a unique rotameric state of W662 at the catalytic site of SARM1. SARM1-IN-10 acts as a paradoxical neurodegeneration inducer at low doses and an inhibitor at high doses, and it can exacerbate or protect against SARM1-mediated neurodegeneration depending on concentration. SARM1-IN-10 can be used in studies of peripheral neurodegeneration.
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- Formule: C25H23FN8
- Masse moléculaire:454.50
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
SARM1-IN-10 (Compound 19) (25 h) protects inducible SAM-TIR HEK293 cells against SARM1-mediated cell death with a pEC50 of 7.8[1].
SARM1-IN-10 (48 h) protects primary rat DRG axons against Vincristine (HY-N0488A)-induced degeneration, with an EC50 of 55 nM[1].
SARM1-IN-10 (48 h) protects primary mouse DRG axons against vincristine-induced degeneration, with an EC50 of 113 nM[1].
Under mild stress conditions, SARM1-IN-10 (overnight) exacerbates CZ-48 (HY-129522)-induced cell death at concentrations below 100 nM, while exerts a protective effect at higher concentrations, in HEK293 cells expressing full-length human SARM1 (without MTS)[1].
At low concentrations, SARM1-IN-10 (9 or 25 h) exacerbates CZ-48-induced axonal degeneration in primary rat DRG under mild stress conditions, while it exerts axon-protective effects at high concentrations[1].
SARM1-IN-10 (49 h) exacerbates vacor-induced axonal degeneration in hiPSC-derived cortical neurons at low concentrations under mild stress conditions, whereas it exerts axonal protective effects at high concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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, 6-to-8 weeks old, spared sciatic nerve injury model)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; twice daily for 4
doses -
Result:Reduced plasma NfL concentrations to levels comparable to the sham group at 50 mg/kg and 100 mg/kg BID.
Increased plasma NfL concentrations relative to the vehicle group at 25 mg/kg BID.
Achieved terminal plasma concentrations of 285 ng/mL at 30 hours (6 hours post-final dose) in the 25 mg/kg group.
Achieved terminal plasma concentrations of 903 ng/mL at 30 hours (6 hours post-final dose) in the 50 mg/kg group.
Achieved terminal plasma concentrations of 3028 ng/mL at 30 hours (6 hours post-final dose) in the 100 mg/kg group.
Chemical Information
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Masse moléculaire 454.50
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Formule C25H23FN8
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SMILES
FC1=CC(N2)=C(C(C#N)=C1)C=C2C3=NC=C(N=C(C4=CC=NC=C4)N5C)C5=C3NCCN(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SARM1-IN-10 Related Classifications
HY-182940 Related Classifications
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