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Nelivaptan

Cat. No. M25410
Nelivaptan Structure
Synonym:

SSR-149415

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Biological Activity

Nelivaptan (SSR-149415) is a vasopressin V1b receptor antagonist.

Chemical Information
Molecular Weight 630.11
Formula C30H32ClN3O8S
CAS Number 439687-69-1
Solubility (25°C) DMSO 60 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] Wenjing Cheng, et al. Neurosci Bull. Paraventricular Nucleus P2X7 Receptors Aggravate Acute Myocardial Infarction Injury via ROS-Induced Vasopressin-V1b Activation in Rats

[2] Jill M Pulley, et al. Future Med Chem. Advocating for mutually beneficial access to shelved compounds

[3] Wafa El-Werfali, et al. Exp Physiol. Haemodynamic and renal sympathetic responses to V1b vasopressin receptor activation within the paraventricular nucleus

[4] Wouter Goutier, et al. Addict Biol. Nicotine-induced locomotor sensitization: pharmacological analyses with candidate smoking cessation aids

[5] Yasukatsu Izumi, et al. J Pharmacol Sci. Therapeutic potential of vasopressin-receptor antagonists in heart failure

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Keywords: Nelivaptan, SSR-149415 supplier, Vasopressin Receptor, inhibitors, activators


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