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RG7713

Cat. No. M11393
RG7713 Structure
Synonym:

RO5028442

Size Price Availability Quantity
5mg USD 425  USD425 In stock
10mg USD 700  USD700 In stock
50mg USD 1950  USD1950 In stock
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Quality Control & Documentation
Biological Activity

RG7713 (RO5028442) is a highly effective and selective brain-osmotic vasopressin 1A (V1a) receptor antagonist with Ki values of 1 nM (hV1a) and 39 nM (mV1a).

Chemical Information
Molecular Weight 437.96
Formula C25H28ClN3O2
CAS Number 920022-47-5
Solubility (25°C) DMSO ≥ 10 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] Daniel Umbricht, et al. Neuropsychopharmacology. A Single Dose, Randomized, Controlled Proof-Of-Mechanism Study of a Novel Vasopressin 1a Receptor Antagonist (RG7713) in High-Functioning Adults with Autism Spectrum Disorder

[2] Daniel Umbricht, et al. Neuropsychopharmacology. A Single Dose, Randomized, Controlled Proof-Of-Mechanism Study of a Novel Vasopressin 1a Receptor Antagonist (RG7713) in High-Functioning Adults with Autism Spectrum Disorder

[3] Hasane Ratni, et al. J Med Chem. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach

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Keywords: RG7713, RO5028442 supplier, Vasopressin Receptor, inhibitors, activators


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