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L-368,899 hydrochloride

Cat. No. M14040
L-368,899 hydrochloride Structure
Size Price Availability
5mg USD 195  USD195 1-2 Weeks
10mg USD 310  USD310 1-2 Weeks
25mg USD 590  USD590 1-2 Weeks
50mg USD 940  USD940 1-2 Weeks
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Quality Control & Documentation
Biological Activity

L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent.

Chemical Information
Molecular Weight 591.23
CAS Number 160312-62-9
Solubility (25°C) DMSO 90 mg/mL
Water 50 mg/mL
Storage 2-8°C, dry, sealed
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] Teruaki Fujitani, et al. Presynaptic glutamatergic transmission and feedback system of oxytocinergic neurons in the hypothalamus of a rat model of adjuvant arthritis

[2] Toshikatsu Okumura, et al. Central oxytocin signaling mediates the central orexin-induced visceral antinociception through the opioid system in conscious rats

[3] Eunice Hagen, et al. Autism-Like Behavior in BTBR Mice Is Improved by Electroconvulsive Therapy

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  Catalog
Abmole Inhibitor Catalog




Keywords: L-368,899 hydrochloride supplier, Oxytocin Receptor, inhibitors, activators


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