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Rodatristat ethyl

Cat. No. M21499
Rodatristat ethyl Structure
Synonym:

KAR5585

Size Price Availability Quantity
5mg USD 920  USD920 In stock
10mg USD 1450  USD1450 In stock
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Quality Control & Documentation
Biological Activity

Rodatristat ethyl (KAR5585) was a first-in-class inhibitor of tryptophan hydroxylase 1 (TPH1) with oral activity.

Chemical Information
Molecular Weight 590.04
Formula C29H31ClF3N5O3
CAS Number 1673571-51-1
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] Howard M Lazarus, et al. Pulm Circ. A trial design to maximize knowledge of the effects of rodatristat ethyl in the treatment of pulmonary arterial hypertension (ELEVATE 2)

[2] David F Condon, et al. Chest. Novel Mechanisms Targeted by Drug Trials in Pulmonary Arterial Hypertension

[3] Daniel R Goldberg, et al. Bioorg Med Chem Lett. Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors

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