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Amiselimod hydrochloride

Cat. No. M7570
Amiselimod hydrochloride Structure
Synonym:

MT-1303 hydrochloride

Size Price Availability Quantity
5mg USD 315  USD350 In stock
10mg USD 432  USD480 In stock
50mg USD 1305  USD1450 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. After oral administration of amiselimod or fingolimod at 1 mg/kg, the concentration of amiselimod-P in rat heart tissue was relatively lower than that of fingolimod-P, potentially contributing to the minimal cardiac effects of amiselimod. Amiselimod-P showed potent selectivity for S1P1 , high selectivity for S1P5 , minimal agonist activity for S1P4 , no distinct agonist activity for S1P2 or S1P3 , and approximately 5-fold weaker GIRK activation than fingolimod-P. Amiselimod 0·2 mg and 0·4 mg significantly reduced the total number of gadolinium-enhanced T1-weighted lesions.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 413.9
Formula C19H31ClF3NO3
CAS Number 942398-84-7
Purity >98%
Solubility 30 mg/mL in DMSO
Storage at -20°C
References

Evaluation and Optimization of in silico designed Sphingosine-1-Phosphate (S1P) Receptor Subtype 1 Modulators for the Management of Multiple Sclerosis.
Gusman DH, et al. Yale J Biol Med. 2017 Mar 29;90(1):15-23. PMID: 28356890.

Cardiac effects of amiselimod compared with fingolimod and placebo: results of a randomised, parallel-group, phase I study in healthy subjects.
Harada T, et al. Br J Clin Pharmacol 2017 May;83(5):1011-1027. PMID: 27921320.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Amiselimod hydrochloride, MT-1303 hydrochloride supplier, S1P Receptor, inhibitors

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