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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Balovaptan (RG7314; RG-7314; RO-5285119) is a novel potent and brain-penetrant vasopressin 1a (hV1a) receptor antagonist with the potential to be used for autism. It inhibits human (hV1a) and mouse (mV1a) receptors with Kis values of 1 and 39 ]nM, respectively. In August 2018, balovaptan began phase 3 clinical development. Balovaptan, however, did not appear to help adults with autism spectrum disorder with their socialization and communication issues, according to a recent report that detailed the outcomes of a phase 3 randomized, placebo-controlled, double-blind clinical trial that was published in Lancet Psychiatry. It can be taken orally once daily and has a half-life of 45–47 hours.
Targets |
hV1a ( Ki = 1 nM ); mV1a ( Ki = 39 nM )
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ln Vitro |
Balovaptan (RG7314) exhibits selectivity for hV1a over hV2 receptors that is >30000-fold, and selectivity over the human oxytocin receptor (hOTR) that is 9891-fold[1].
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References |
Molecular Formula |
C22H24CLN5O
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Molecular Weight |
409.918
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Exact Mass |
409.17
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Elemental Analysis |
C, 64.46; H, 5.90; Cl, 8.65; N, 17.09; O, 3.90
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CAS # |
1228088-30-9
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Appearance |
Solid powder
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SMILES |
CN1CC2=C(C=CC(=C2)Cl)N3C(=NN=C3C4CCC(CC4)OC5=CC=CC=N5)C1
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InChi Key |
GMPZPHGHNDMRKL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H24ClN5O/c1-27-13-16-12-17(23)7-10-19(16)28-20(14-27)25-26-22(28)15-5-8-18(9-6-15)29-21-4-2-3-11-24-21/h2-4,7,10-12,15,18H,5-6,8-9,13-14H2,1H3
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Chemical Name |
8-chloro-5-methyl-1-(4-pyridin-2-yloxycyclohexyl)-4,6-dihydro-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
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Synonyms |
RG7314; RG-7314; RO-5285119; RG 7314; RO5285119
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~50 mg/mL (~122.0 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4395 mL | 12.1975 mL | 24.3950 mL | |
5 mM | 0.4879 mL | 2.4395 mL | 4.8790 mL | |
10 mM | 0.2440 mL | 1.2198 mL | 2.4395 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03764449 | Completed | Drug: Oral Balovaptan Drug: IV Balovaptan |
Healthy Volunteers | Hoffmann-La Roche | January 10, 2019 | Phase 1 |
NCT04156646 | Recruiting | Drug: Balovaptan Drug: Esomeprazole |
Autism Spectrum Disorder | Hoffmann-La Roche | November 19, 2019 | Phase 1 |
NCT03579719 | Completed | Drug: Balovaptan Drug: Itraconazole |
Healthy Volunteers | Hoffmann-La Roche | July 10, 2018 | Phase 1 |
NCT05401565 | Completed | Drug: Balovaptan Drug: Placebo |
Stress Disorders, Post-Traumatic | Hoffmann-La Roche | August 2, 2022 | Phase 2 |