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| 25mg |
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| Targets |
L-371,257 targets the oxytocin receptor (OTR) and the vasopressin V1a receptor. As a competitive antagonist, it binds to these receptors and blocks the binding of their endogenous ligands, oxytocin and vasopressin, respectively. It has a pA₂ of 8.4 and a Ki of 19 nM at the OTR, and a Ki of 3.7 nM at the V1a receptor. Its selectivity for the OTR over V1a and V2 is >800-fold.
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| ln Vitro |
In vitro, L-371,257 is a potent antagonist of the oxytocin receptor with a pA₂ of 8.4 and a Ki of 19 nM. It also shows high affinity for the vasopressin V1a receptor with a Ki of 3.7 nM. Its selectivity for the OTR over V1a and V2 is >800-fold. These in vitro activities confirm its potent antagonism and selectivity profile.
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| 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].
Detailed in vivo activity data for L-371,257 are not extensively reported in the available literature. However, as an orally bioavailable, non-BBB penetrant antagonist, it is expected to have peripheral effects, making it useful for studying the peripheral roles of oxytocin and vasopressin. Its applications include research on these receptors in peripheral tissues. |
| Enzyme Assay |
Non-cell-based receptor binding assays for L-371,257 involve radioligand binding studies using membrane preparations from cells expressing the oxytocin or vasopressin V1a receptors. The receptor is incubated with a radiolabeled ligand and varying concentrations of L-371,257. Its binding affinity (Ki) is determined by measuring the displacement of the radiolabeled ligand, with values of 19 nM for OTR and 3.7 nM for V1a.
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| Cell Assay |
Cellular assays for L-371,257 are performed using cells expressing the oxytocin or vasopressin V1a receptors. Cells are treated with the compound at various concentrations, followed by stimulation with the appropriate agonist. Downstream signaling, such as calcium mobilization, is measured. The compound's ability to inhibit agonist-stimulated signaling is quantified. IC₅₀ or pA₂ values are determined.
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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). In vivo animal models for L-371,257 would be required to assess its therapeutic potential. Based on its mechanism as an OTR and V1a antagonist, relevant models could include those for preterm labor, social behavior, or cardiovascular function. The compound would be administered orally, and relevant physiological or behavioral parameters would be measured. |
| ADME/Pharmacokinetics |
L-371,257 has a molecular weight of 519.59 g/mol and a molecular formula of C₂₈H₃₃N₃O₆. Its CAS number is 162042-44-6. The compound is supplied as a solid with a purity of >98%. It is soluble in DMSO. Storage conditions: -20°C. The compound is an orally bioavailable, non-BBB penetrant OTR antagonist. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for L-371,257 are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, competitive, and selective antagonist of the oxytocin receptor. It has a pA₂ of 8.4 and a Ki of 19 nM for OTR, and a Ki of 3.7 nM for vasopressin V1a. It displays >800-fold selectivity over V1a and V2. Its CAS number is 162042-44-6.
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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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