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ML-SI3

Cat. No. M20832
ML-SI3 Structure
Size Price Availability Quantity
5mg USD 160  USD160 In stock
10mg USD 260  USD260 In stock
25mg USD 480  USD480 In stock
50mg USD 720  USD720 In stock
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Quality Control & Documentation
Biological Activity

ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.

Chemical Information
Molecular Weight 429.58
Formula C23H31N3O3S
CAS Number 891016-02-7
Form Solid
Solubility (25°C) DMSO 43 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Maike R Pollmanns, et al. Front Cell Neurosci. Activated Endolysosomal Cation Channel TRPML1 Facilitates Maturation of α-Synuclein-Containing Autophagosomes

[2] Katharina Kriegler, et al. Arch Pharm (Weinheim). Effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans-ML-SI3

[3] Philip Schmiege, et al. Structure. Atomic insights into ML-SI3 mediated human TRPML1 inhibition

[4] Charlotte Leser, et al. Eur J Med Chem. Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3

[5] Dan Li, et al. Autophagy. Sulforaphane Activates a lysosome-dependent transcriptional program to mitigate oxidative stress

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Keywords: ML-SI3 supplier, TRP Channel, inhibitors, activators


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