L-372662 |
| رقم الكتالوجGC63036 |
L-372662 هو أحد مضادات الأوكسيتوسين غير الببتيدية الفعالة عن طريق الفم مع قيمة Ki 4.8
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 162045-26-3
Sample solution is provided at 25 µL, 10mM.
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L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR[1][2].
L-372662 is an antagonist of oxytocin-induced uterine contractions in late gestation pregnant rhesus monkeys (AD50 = 36 micrograms/kg), oral bioavailability (F = 90% in dogs), and aqueous solubility (10 mg/mL).
[1]. Bell, I. M., Erb, J. M., Freidinger, R. M., Gallicchio, S. N., Guare, J. P., Guidotti, M. T., … Woyden, C. J. (1998). Development of Orally Active Oxytocin Antagonists: Studies on 1-(1-{4-[1-(2-Methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl}piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and Related Pyridines. Journal of Medicinal Chemistry, 41(12), 2146-2163.
[2]. Hawtin SR, et al. A Gly/Ala switch contributes to high affinity binding of benzoxazinone-based non-peptide oxytocin receptor antagonists. FEBS Lett. 2005;579(2):349-356.
[3]. Williams PD, et al. Progress in the development of oxytocin antagonists for use in preterm labor. Adv Exp Med Biol. 1998;449:473-479.
| Cas No. | 162045-26-3 | SDF | |
| Formula | C33H38N4O6 | M.Wt | 586.68 |
| الذوبان | DMSO : 100 mg/mL (170.45 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7045 mL | 8.5225 mL | 17.0451 mL |
| 5 mM | 0.3409 mL | 1.7045 mL | 3.409 mL |
| 10 mM | 0.1705 mL | 0.8523 mL | 1.7045 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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