2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. SARM1-IN-7

SARM1-IN-7 is a potent active site (orthosteric) and orally active SARM1 inhibitor. SARM1-IN-7 continuously activates the enzymatic activity of SARM1, thereby exacerbating the depletion of NAD at sub-minimal concentrations. SARM1-IN-7 demonstrated dual benefits in the SARM1-activated cell models and mouse models: a high dose exerted a cell/neuron protective effect, while a low dose exacerbated cell/neuron damage. SARM1-IN-7 can be used for the study of axon degeneration.

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SARM1-IN-7

SARM1-IN-7 Chemical Structure

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SARM1-IN-7 Related Antibodies

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Description

SARM1-IN-7 is a potent active site (orthosteric) and orally active SARM1 inhibitor. SARM1-IN-7 continuously activates the enzymatic activity of SARM1, thereby exacerbating the depletion of NAD at sub-minimal concentrations. SARM1-IN-7 demonstrated dual benefits in the SARM1-activated cell models and mouse models: a high dose exerted a cell/neuron protective effect, while a low dose exacerbated cell/neuron damage. SARM1-IN-7 can be used for the study of axon degeneration[1].

In Vitro

EGFR-IN-172 (Compound NB-3) (0.06 nM-0.6 μM, 24 h) inhibits SARM1 at high concentrations, thereby rescuing cell viability, but subinhibitory concentrations of BEIs potentiated SARM1-induced cell death in SH-SY5Y cells[1].

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

SARM1-IN-7 Related Antibodies
In Vivo

SARM1-IN-7 (Compound NB-3) (0.3-30 mg/kg, i.g., single dose or two doses) significantly reduces the level of plasma NfL at high dose but the low dose exacerbates nerve damage, leading to adverse events such as drowsiness, immobility, and even death in the mouse model of SARM1 activation induced by Vacor, and the same results is observed in the low-dose Vacor model and the sciatic nerve transection (SNT) model[1].

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

Animal Model: Vacor (30mg/kg and 50 mg/kg) induced SARM1 activation model established in 9-10 week old male and female mice (C57bl/6 J)[1]
Dosage: 0.3, 3 and 30 mg/kg (50 mg/kg Vacor model); 0.3 and 1 mg/kg (30mg/kg Vacor model)
Administration: Oral gavage (i.g.), 2 doses (1 hour before the administration of Vacor and 8 hours after the first administration)
Result: Significantly reduced the level of plasma NfL at high dose.
Caused exacerbates nerve damage, leading to adverse events such as drowsiness, immobility, and even death at low doses.
Did not cause nerve damage or adverse events use alone.
Animal Model: Sciatic nerve transection (SNT) model established in 9-10 week old male and female mice (C57bl/6 J)[1]
Dosage: 0.3, 1 and 30 mg/kg
Administration: Oral gavage (i.g.), single dose
Result: Observed the same phenomenon.
Molecular Weight

247.22

Formula

C10H12F3N3O
SMILES

C[C@H](N(C)C(NC(F)(F)F)=O)C1=CC=NC=C1
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-7 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-7Toll-like Receptor (TLR)SARM1NADaseNeurodegenerationAxon DegenerationBase-Exchange Inhibitors (BEIs)Paradoxical ActivationSubinhibitory ConcentrationsNeurofilament Light Chain (NfL)VacorAdverse EventsInhibitorinhibitorinhibit

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HY-175879
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