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AM095 sodium

Cat. No. M7674
AM095 sodium Structure
Synonym:

AM095

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 190  USD190 In stock
50mg USD 575  USD575 In stock
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Quality Control & Documentation
Biological Activity

AM095 is a potent and selective, orally bioavailable antagonist of lysophosphatidic acid receptor1 (LPA1). AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM). LPA1 has been shown to be involved in neuropathic pain. AM095 inhibition of LPA1 after spinal cord injury resulted in reduced demyelination and improvement in locomotor recovery.

Chemical Information
Molecular Weight 478.47
Formula C27H23N2NaO5
CAS Number 1345614-59-6
Solubility (25°C) DMSO: ≥ 50 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] Castelino FV, et al. Arthritis Rheum. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma.

[2] Swaney JS, et al. J Pharmacol Exp Ther. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist.

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