| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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L-371,257 (L371,257) is a novel and potent non-peptide oxytocin (OT) receptor antagonist (pA2=8.4). It exhibits high affinity against oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
| ln Vivo |
Body weight growth is stimulated by systemic injection of the non-osmotic oxytocin receptor antagonist L-371,257 (0.5 and 1.0 mg/kg; i.p.) [3].
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| Animal Protocol |
Animal/Disease Models: Six-hour fasted rats [3]
Doses: 0.5 and 1.0 mg/kg Route of Administration: intraperitoneal (ip) injection (single) at the beginning of the dark cycle and 30-45 minutes before eating; intraperitoneal (ip) injection (repeated injection) for 6 days. Experimental Results: Single injections of 0.5 and 1.0 mg/kg Dramatically stimulated weight gain relative to vehicle treatment. When repeated over 6 days, 0.5 mg/kg Dramatically stimulated body weight gain (10.5±2.2 g) relative to vehicle treatment (4.7±2.7 g). |
| References |
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| Molecular Formula |
C28H33N3O6
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|---|---|
| Molecular Weight |
507.59
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| Exact Mass |
507.237
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| Elemental Analysis |
C, 66.26; H, 6.55; N, 8.28; O, 18.91
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| CAS # |
162042-44-6
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| PubChem CID |
6918320
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| Appearance |
White to off-white solid powder
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| LogP |
3.787
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
37
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| Complexity |
823
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=O)N1CCC(CC1)OC2=CC(=C(C=C2)C(=O)N3CCC(CC3)N4C5=CC=CC=C5COC4=O)OC
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| Synonyms |
L371,257 L 371,257 L-371,257
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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 : ~8.33 mg/mL (~16.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.64 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (1.64 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 8.3 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: ≥ 0.83 mg/mL (1.64 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 | 1.9701 mL | 9.8505 mL | 19.7009 mL | |
| 5 mM | 0.3940 mL | 1.9701 mL | 3.9402 mL | |
| 10 mM | 0.1970 mL | 0.9850 mL | 1.9701 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.
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