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Balovaptan

Cat. No. M21942
Balovaptan Structure
Synonym:

RG7314

Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 118  USD118 In stock
25mg USD 235  USD235 In stock
50mg USD 360  USD360 In stock
100mg USD 595  USD595 In stock
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Quality Control & Documentation
Biological Activity

Balovaptan (RG7314) is an orally available, selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors. Balovaptan (RG7314) is used for the research of autism.

Chemical Information
Molecular Weight 409.91
Formula C22H24ClN5O
CAS Number 1228088-30-9
Solubility (25°C) DMSO 45 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] Eric Hollander, et al. JAMA Psychiatry. Balovaptan vs Placebo for Social Communication in Childhood Autism Spectrum Disorder: A Randomized Clinical Trial

[2] Suma Jacob, et al. Mol Autism. Large multicenter randomized trials in autism: key insights gained from the balovaptan clinical development program

[3] Suma Jacob, et al. Lancet Psychiatry. Efficacy and safety of balovaptan for socialisation and communication difficulties in autistic adults in North America and Europe: a phase 3, randomised, placebo-controlled trial

[4] Michael Derks, et al. Expert Opin Investig Drugs. Bioavailability and pharmacokinetic profile of balovaptan, a selective, brain-penetrant vasopressin 1a receptor antagonist, in healthy volunteers

[5] Michael G M Derks, et al. Adv Ther. Open-Label Assessment of the Effects of Itraconazole and Rifampicin on Balovaptan Pharmacokinetics in Healthy Volunteers

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Keywords: Balovaptan, RG7314 supplier, Vasopressin Receptor, inhibitors, activators


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