1. GPCR/G Protein
  2. Vasopressin Receptor
  3. RG7713

RG7713 (Synonyms: RO5028442)

Cat. No.: HY-12981 Purity: 99.79%
Handling Instructions

RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

For research use only. We do not sell to patients.

RG7713 Chemical Structure

RG7713 Chemical Structure

CAS No. : 920022-47-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

IC50 & Target

Ki: 1 nM (hV1a receptor), 39 nM (mV1a receptor)[1]

In Vitro

RG7713 (RO5028442) (compound 8) has excellent binding in and functional affinity for hV1a, moderate mouse affinity, and excellent selectivity versus human V2 (hV2) and human oxytocin (hOT) receptors. RG7713 (RO5028442) shows high solubility. RG7713 (RO5028442) is found to be highly selective against a panel of 89 targets. Finally, RG7713 (RO5028442) is identified as a suitable compound for clinical studies[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

437.96

Formula

C₂₅H₂₈ClN₃O₂

CAS No.

920022-47-5

SMILES

O=C(C1=CN(CCN(C)C)C2=C1C=CC(Cl)=C2)N3CCC4(C(C=CC=C5)=C5CO4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (45.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2833 mL 11.4166 mL 22.8331 mL
5 mM 0.4567 mL 2.2833 mL 4.5666 mL
10 mM 0.2283 mL 1.1417 mL 2.2833 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (4.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (4.57 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (4.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

CHO cells are stably transfected with expression plasmids encoding human V1a and grown in F-12 K, containing 10% fetal bovine serum, 1% penicillin-streptomycin, 1% glutamate, and 200 μg/mL geneticin at 37 °C in a 10% CO2 incubator at 95% humidity. Cells are plated for 24 h at 50,000 cells/well in clear bottomed 96 well plates and are dye loaded for 60 min with 2 μM Fluo-4-AM in assay buffer. After cell washing, the plate is loaded on a fluorometric imaging plate reader, compound dilution series added to the cells, and agonist activity measured[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

RG7713RO5028442RG 7713RG-7713RO 5028442RO-5028442Vasopressin ReceptorInhibitorinhibitorinhibit

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Product Name:
RG7713
Cat. No.:
HY-12981
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