2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. 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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SARM1-IN-10

SARM1-IN-10 Chemical Structure

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SARM1-IN-10 Related Antibodies

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Description

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[1].

In Vitro

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.

SARM1-IN-10 Related Antibodies
Parmacokinetics
Species Dose Route CL CLunbound Vd T1/2 Bioavailability
Mice[1] 2 mg/kg i.v. 50 mL/min/kg 417 mL/min/kg 5.0 L/kg 1.1 h /
Mice[1] 5 mg/kg p.o. / / / / 34 %
In Vivo

SARM1-IN-10 (Compound 19) (25-100 mg/kg; p.o.; twice daily for a total of 4 doses) exerts a neuroprotective effect against neurodegeneration in mouse models, but increases the levels of neurodegeneration-related biomarkers at low doses[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 6-to-8 weeks old, spared sciatic nerve injury model)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
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.
Molecular Weight

454.50

Formula

C25H23FN8
SMILES

FC1=CC(N2)=C(C(C#N)=C1)C=C2C3=NC=C(N=C(C4=CC=NC=C4)N5C)C5=C3NCCN(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SARM1-IN-10 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SARM1-IN-10Toll-like Receptor (TLR)mouse SNI modelSARM1 TIR domainW662NAD+rat DRG axonsSARM1hiPSC-derived cortical neuronsHEK293 cellsmouse DRG axonsperipheral nerve degenerationInhibitorinhibitorinhibit

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