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SRX246 

Cat. No. M30218
SRX246  Structure
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Biological Activity

SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.

Chemical Information
Molecular Weight 703.87
Formula C42H49N5O5
CAS Number 512784-93-9
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
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] Hilda T Maibach, et al. J Pers Med. The Vasopressin 1a Receptor Antagonist SRX246 Reduces Aggressive Behavior in Huntington's Disease

[2] Tiffany R Lago, et al. Psychopharmacology (Berl). The novel vasopressin receptor (V1aR) antagonist SRX246 reduces anxiety in an experimental model in humans: a randomized proof-of-concept study

[3] Michael J Brownstein, et al. J Clin Med. Safety and Tolerability of SRX246, a Vasopressin 1a Antagonist, in Irritable Huntington's Disease Patients-A Randomized Phase 2 Clinical Trial

[4] Royce J Lee, et al. Front Syst Neurosci. A novel V1a receptor antagonist blocks vasopressin-induced changes in the CNS response to emotional stimuli: an fMRI study

[5] Karine M Fabio, et al. J Pharm Sci. Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist

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Keywords: SRX246  supplier, Vasopressin Receptor, inhibitors, activators

 
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